Papers Archives - Sophion

A Microscopy-Based Small Molecule Screen in Primary Neurons Reveals Neuroprotective Properties of the FDA-Approved Anti-Viral Drug Elvitegravir

Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors

Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ1 Receptor Antagonist Clinical Candidate for the Treatment of Pain

Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency

Characterisation of δ-Conotoxin TxVIA as a Mammalian T-Type Calcium Channel Modulator

Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria

Recombinant Production , Bioconjugation and Membrane Binding Studies of Pn3a , a Selective Nav1.7 Inhibitor

Discovery, Pharmacological Characterisation and NMR Structure of the Novel µ-Conotoxin SxIIIC, a Potent and Irreversible NaV Channel Inhibitor

Cannabidiol Inhibits Multiple Cardiac Ion Channels and Shortens Ventricular Action Potential Duration in Vitro

In Vitro and in Vivo Characterization of Lu AA41178: A Novel, Brain Penetrant, Pan-Selective Kv7 Potassium Channel Opener with Efficacy in Preclinical Models of Epileptic Seizures and Psychiatric Disorders

Inhibitory Effect of Anti-Seizure Medications on Ionotropic Glutamate Receptors: Special Focus on AMPA Receptor Subunits

New V1a Receptor Antagonist. Part 2. Identification and Optimization of Triazolobenzazepines

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators

Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel Nav1.7 Inhibition

A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair

Modulation of Lymphocyte Potassium Channel KV1.3 by Membrane-Penetrating, Joint-Targeting Immunomodulatory Plant Defensin

Novel bacterial topoisomerase inhibitors derived from isomannide

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I

Ion Channels and Relevant Drug Screening Approaches

Design, Synthesis and Biological Activity of Novel 2,3,4,5-Tetra-Substituted Thiophene Derivatives as PI3Kα Inhibitors with Potent Antitumor Activity

Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome

Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity

Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs

Characterization of Synthetic Tf2 as a Nav1.3 Selective Pharmacological Probe

Antimicrobial Peptides from Rat-Tailed Maggots of the Drone Fly Eristalis tenax Show Potent Activity against Multidrug-Resistant Gram-Negative Bacteria

Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors

Fluorescence labeling of a Nav1.7-targeted peptide for near-infrared nerve visualization

Inhibition of KCa2 Channels Decreased the Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced Hypokalemia

A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy

Development of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves

Recombinant production, bioconjugation and membrane binding studies of Pn3a, a selective Nav1.7 inhibitor

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators

Electrophysiological Studies of GABA-A Receptors Using QPatch II, the Next Generation of Automated Patch‐Clamp Instruments

A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair

Screening Assay Protocols Targeting the Nav1.7 Channel Using Qube High‐Throughput Automated Patch‐Clamp System

Modulation of Lymphocyte Potassium Channel Kv1.3 by Membrane-Penetrating, Joint-Targeting Immunomodulatory Plant Defensin

Novel bacterial topoisomerase inhibitors derived from isomannide

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I

Ion Channels and Relevant Drug Screening Approaches

Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity

Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome

Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity

Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs

Characterization of Synthetic Tf2 as a Nav1.3 Selective Pharmacological Probe

Antimicrobial Peptides from Rat-Tailed Maggots of the Drone Fly Eristalis tenax Show Potent Activity against Multidrug-Resistant Gram-Negative Bacteria

Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors

Fluorescence labeling of a Nav1.7-targeted peptide for near-infrared nerve visualization

Inhibition of KCa2 Channels Decreased the Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced Hypokalemia

A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy

Development of a selective inhibitor for Kv1.1 channels prevalent in demyelinated nerves

Mapping the Molecular Surface of the Analgesic Nav1.7-Selective Peptide Pn3a Reveals Residues Essential for Membrane and Channel Interactions

Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs

Put a cork in it: Plugging the M2 viral ion channel to sink influenza.

TMEM16A Potentiation: A Novel Therapeutic Approach for the Treatment of Cystic Fibrosis

In vitro characterization of the thermoneutral transient receptor potential vanilloid-1 (TRPV1) inhibitor GRTE16523

Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned

Manipulation of a spider peptide toxin alters its affinity for lipid bilayers and potency and selectivity for voltage-gated sodium channel subtype

A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm

Screening assay protocols targeting the Nav1.7 Channel using Qube, a high-throughput automated patch clamp system

Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells

Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile

Wnts control membrane potential in mammalian cancer cells

Cardiac safety assessment with motion field imaging analysis of human iPS cell-derived cardiomyocytes is improved by an integrated evaluation with cardiac ion channel profiling

Role of High-Throughput Electrophysiology in Drug Discovery

Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel Nav1.7 Inhibition

Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel NaV1.1 Provide Novel Leads for Development of Antiepileptic Drugs

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation

Synthesis and Biological Evaluation of Five‐Atom‐Linker‐Based Arylpiperazine Derivatives with an Atypical Antipsychotic Profile

Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems

Extracellular K+ Dampens T Cell Functions: Implications for Immune Suppression in the Tumor Microenvironment

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain

Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination

Development of a high-throughput fluorescent no-wash sodium influx assay

From identification to functional characterization of cyriotoxin-1a, an antinociceptive toxin from the spider Cyriopagopus schioedtei.

Simultaneous assessment of compound activity on cardiac Nav1.5 peak and late currents in an automated patch clamp platform

Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination

Electrophysiological and Pharmacological Characterization of Human Inwardly Rectifying Kir2.1 Channels on an Automated Patch-Clamp Platform

Novel Chitohexaose Analog Protects Young and Aged mice from CLP Induced Polymicrobial Sepsis

Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide are Potent TMEM16A Antagonists that Fully Bronchodilate Airway

Differential Free Intracellular Calcium Release by Class II Antiarrhythmics in Cancer Cell Lines

Benzothiophenes as Potent Analgesics Against Neuropathic Pain

Development of the 1,2,4-triazole-based anticonvulsant drug candidates acting on the voltage-gated sodium channels. Insights from in-vivo, in-vitro, and in-silico studies

Synthesis of Pseudellone Analogs and Characterization as Novel T-type Calcium Channel Blockers

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel

Biological Profiling of Coleoptericins and Coleoptericin-Like Antimicrobial Peptides from the Invasive Harlequin Ladybird Harmonia axyridis

Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain

Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis

Selective Nav1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

Inhibitory effects of cannabidiol on voltage-dependent sodium currents

A comprehensive portrait of the venom of the giant red bull ant, Myrmecia gulosa, reveals a hyperdiverse hymenopteran toxin gene family

Discovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.

Screening strategies for the discovery of ion channel monoclonal antibodies

Efficient Enzymatic Ligation of Inhibitor Cystine Knot Spider Venom Peptides: Using Sortase A To Form Double-Knottins That Probe Voltage-Gated Sodium Channel NaV1.7

Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect

GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P ) channel opener, reduces rat dorsal root ganglion neuron excitability

The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6

Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy

Direct evidence for high affinity blockade of NaV1.6 channel subtype by huwentoxin-IV spider peptide, using multiscale functional approaches

Co-expression of β Subunits with the Voltage-Gated Sodium Channel NaV1.7: the Importance of Subunit Association and Phosphorylation and Their Effects on Channel Pharmacology and Biophysics

4-Substituted carbamazepine derivatives: conformational analysis and sodium channel-blocking properties

Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp

A Small Molecule Induces Oligodendrogenesis Leading to Myelin Sheath Repair

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis

A dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a P2X7 antagonist clinical candidate

Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells: An In-Vitro Model to Predict Cardiac Effects of Drugs

The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6+/− mice

Eleclazine exhibits enhanced selectivity for long QT syndrome type 3–associated late Na+ current

Termination of Vernakalant-Resistant Atrial Fibrillation by Inhibition of Small-Conductance Ca2+-Activated K+ Channels in Pigs

Cardiac sodium channel antagonism – Translation of preclinical in vitro assays to clinical QRS prolongation

Discovery and electrophysiological characterization of SKF-32802; a novel hERG agonist found through a large-scale structural similarity search

Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels

Design, synthesis and biological evaluation of 4,7,12,12a-tetrahydro-5H-thieno[3′,2’:3,4]pyrido[1,2-b]isoquinolines as novel adenosine 5′-monophosphate-activated protein kinase (AMPK) indirect activators for the treatment of type 2 diabetes

Discovery and mode of action of a novel analgesic β-toxin from the African spider Ceratogyrus darlingi

Pharmacological screening technologies for venom peptide discovery

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

An Official American Thoracic Society Workshop Report: Translational Research in Rare Respiratory Diseases

Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors

Using automated patch clamp electrophysiology platforms in pain-related ion channel research: insights from industry and academia

A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo

Effect of antiarrhythmic drugs on small conductance calcium – activated potassium channels

Intracellular Calcium Mobilization in Response to Ion Channel Regulators via a Calcium-Induced Calcium Release Mechanism

NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions

Development of Automated Patch Clamp Technique to Investigate CFTR Chloride Channel Function

Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling

Automated and manual patch clamp data of human induced pluripotent stem cell-derived dopaminergic neurons

Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium

Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels

Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr–/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator

High throughput physiological screening of iPSC-derived cardiomyocytes for drug development