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List of works by Paul C. Levesque

7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site

scientific article published on September 24, 2011

A New Perspective in the Field of Cardiac Safety Testing through the Comprehensive In Vitro Proarrhythmia Assay Paradigm.

scientific article published on 13 July 2015

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

scientific article published on 21 March 2020

ATPo but not cAMPi activates a chloride conductance in mouse ventricular myocytes

scientific article published on 01 March 1995

Alternative splicing of CFTR Cl- channels in heart ⬇️

scientific article published on 01 June 1993

Anion and cation modulation of the guinea-pig ventricular action potential during beta-adrenoceptor stimulation

scientific article published on 01 June 1993

Antiarrhythmic drug therapy for atrial fibrillation: focus on atrial selectivity and safety

scientific article published on January 2009

Aryl Ether-Derived Sphingosine-1-Phosphate Receptor (S1P1) Modulators: Optimization of the PK, PD, and Safety Profiles

scientific article published on 11 August 2020

Assessing seizure liability using multi-electrode arrays (MEA)

scientific article published on 04 December 2018

Benzopyran sulfonamides as KV1.5 potassium channel blockers

scientific article published on 10 April 2007

Characterization of contractile properties of hIPSC-CMs cultured with or without fibroblast and chronic electrical stimulation

scientific article published on 01 September 2019

Comparative electrophysiology and pharmacology of hiPSC cardiomyocyte 2D mono-cultures and 2D co-cultures with human ventricular fibroblasts

scientific article published on 01 September 2019

Corrigendum to "A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm" [Toxicology and Applied Pharmacology volume 394C (2020) 114961]

scientific article published on 02 April 2020

Cross-Site Reliability of Human Induced Pluripotent Stem-Cell Derived Cardiomyocyte Based Safety Assays using Microelectrode Arrays: Results from a Blinded CiPA Pilot Study

scientific article published on 27 April 2018

Cystic fibrosis gene encodes a cAMP-dependent chloride channel in heart

scientific article published on June 1996

Design and Synthesis of 4-Substituted Benzamides as Potent, Selective, and Orally Bioavailable IKs Blockers ⬇️

scientific article published on November 8, 2001

Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors

scientific article published on 20 May 2014

Development of a chemiluminescent ELISA method for the detection of total anti-Adeno Associated Virus Serotype 9 (AAV9) antibodies

article

Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)).

scientific article

Dihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists

scientific article

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

scientific article published on 16 June 2016

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection

scientific article

Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor

scientific article

Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor

scientific article published on 06 May 2019

Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing

scientific article published on 26 August 2016

Dominant-Negative KvLQT1 Mutations Underlie the LQT1 Form of Long QT Syndrome ⬇️

scientific article published on September 16, 1997

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists.

scientific article

Estimation of hERG inhibition of drug candidates using multivariate property and pharmacophore SAR.

scientific article published on 14 June 2007

Evaluating the use of microelectrode array technology and cell-based neuronal culture models for proconvulsant risk assessment: progress from the HESI NeuTox consortium

scientific article published on 01 September 2019

Evaluation of cardiac function in unrestrained dogs and monkeys using left ventricular dP/dt

scientific article published on 08 April 2016

Expression and characterization of human transient receptor potential melastatin 3 (hTRPM3).

scientific article published on 2 April 2003

Expression of cystic fibrosis transmembrane regulator Cl- channels in heart

scientific article published on October 1, 1992

Functional Expression of Two KvLQT1-related Potassium Channels Responsible for an Inherited Idiopathic Epilepsy ⬇️

scientific article published on July 31, 1998

How do the top 12 pharmaceutical companies operate safety pharmacology? ⬇️

scientific article published on April 1, 2012

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into

scientific article published on 06 March 2019

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials

scientific article published on 19 January 2016

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antipla

scientific article published on 31 January 2014

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

scientific article

Identification of potent tricyclic prodrug S1P1 receptor modulators

scientific article published on 25 November 2016

LC/MS/MS-based Quantitation of Pig and Human S100A1 Protein in Cardiac Tissues: Application to Gene Therapy

scientific article published on 07 May 2020

Molecular physiology of CFTR Cl- channels in heart.

scientific article published in January 1994

Position 5.46 of the serotonin 5-HT2A receptor contributes to a species-dependent variation for the 5-HT2C agonist (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one: impact on selectivity and toxicological evaluatio

scientific article published on 18 September 2009

Pseudosaccharin amines as potent and selective KV1.5 blockers

scientific article published on 07 March 2015

Pyrano-[2,3b]-pyridines as potassium channel antagonists

scientific article

Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers

scientific article published on 4 January 2010

Release of calcium from guinea pig cardiac sarcoplasmic reticulum induced by sodium-calcium exchange

scientific article

Renal studies in safety pharmacology and toxicology: A survey conducted in the top 15 pharmaceutical companies

scientific article published on 29 January 2015

Role of T-type calcium channel subunits in post-myocardial infarction remodelling probed with genetically engineered mice.

scientific article published on 27 May 2011

Role of reverse-mode Na(+)-Ca2+ exchange in excitation-contraction coupling in the heart

scientific article

Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide.

scientific article

Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus.

scientific article published on 9 December 2016

Tetrahydronaphthalene-derived amino alcohols and amino ketones as potent and selective inhibitors of the delayed rectifier potassium current IKs.

scientific article published in January 2004

The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection

scientific article published on 5 March 2014

Time for a Fully Integrated Nonclinical-Clinical Risk Assessment to Streamline QT Prolongation Liability Determinations: A Pharma Industry Perspective

scientific article published on 31 August 2020

Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists ⬇️

scientific article published on January 26, 2013

Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-79531

scientific article published on 2 November 2015

Unitary Cl- channels activated by cytoplasmic Ca2+ in canine ventricular myocytes

scientific article published in May 1996

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