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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I Nai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9005-9017

2016

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Drug Annotations Series Change in Guidelines

Journal of medicinal chemistry, 2019-03, Vol.62 (5), p.2217-2217

2019

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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3202-3206

2016

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Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII)

Bioorganic & medicinal chemistry letters, 2018-02, Vol.28 (3), p.541-546

2018

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Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists

The Journal of pharmacology and experimental therapeutics, 2001-07, Vol.298 (1), p.209

2001

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CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability

Bioorganic & medicinal chemistry letters, 2004-12, Vol.14 (24), p.6017-6021

2004

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Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (14), p.3793-3797

2004

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Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Bioorganic & medicinal chemistry letters, 2004-01, Vol.14 (2), p.535-539

2004

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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late I Na i) of the cardiac Na v 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3207-3211

2016

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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late I Na i) of the cardiac Na V 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3202-3206

2016

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Using Patchxpress to Screen Blockers of the Cardiac Sodium Channel (Nav1.5) for Effects on Late INA, Peak INA, and Channel Kinetics

Biophysical journal, 2010-01, Vol.98 (3), p.113a-113a

2010

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Partial A(1) adenosine receptor agonists from a molecular perspective and their potential use as chronic ventricular rate control agents during atrial fibrillation (AF)

Current topics in medicinal chemistry, 2004, Vol.4 (8), p.839

2004

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Affinity and intrinsic efficacy (IE) of 5′-carbamoyl adenosine analogues for the A 1 adenosine receptor—efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Bioorganic & medicinal chemistry letters, 2004, Vol.14 (2), p.535-539

2004

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Structure–affinity relationships of 5 ′ -aromatic ethers and 5 ′ -aromatic sulfides as partial A 1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (14), p.3793-3797

2004

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CVT-4325: A Potent Fatty Acid Oxidation Inhibitor with Favorable Oral Bioavailability

ChemInform, 2005-04, Vol.36 (15), p.no-no

2005

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Structure‐Affinity Relationships of the Affinity of 2‐Pyrazolyl Adenosine Analogues for the Adenosine A 2A Receptor

ChemInform, 2003-02, Vol.34 (8)

2003

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A1 adenosine receptor agonists and their potential therapeutic applications

Expert opinion on investigational drugs, 2008-12, Vol.17 (12), p.1901-1910

2008

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A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias

The Journal of pharmacology and experimental therapeutics, 2013-01, Vol.344 (1), p.23

2013

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Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi

Bioorganic & medicinal chemistry letters, 2019-08, Vol.29 (16), p.2428-2436

2019

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Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B

Journal of medicinal chemistry, 2020-09, Vol.63 (18), p.10188-10203

2020

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The Drug Annotations Series

Journal of medicinal chemistry, 2013-09, Vol.56 (17), p.6541-6541

2013

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Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (24), p.5926-5930

2016

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Molecule Evoluator CIDRUX BV, Park Oosterspaarn 6, 2036 MB Haarlem, The Netherlands. www. cidrux.com. See Web site for pricing information

Journal of the American Chemical Society, 2007-10, Vol.129 (41), p.12586-12586

Zablocki, Jeff

2007

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Marked difference in saxitoxin and tetrodoxin affinity for the human nociceptive voltage-gated sodium channel (Naᵥ1.7)

Proceedings of the National Academy of Sciences - PNAS, 2012-10, Vol.109 (44), p.18102-18107

2012

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A1 adenosine receptor antagonists, agonists, and allosteric enhancers

Handbook of experimental pharmacology, 2009 (193), p.25

2009

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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I Nai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Drug Annotations Series Change in Guidelines

Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine

Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII)

Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists

CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability

Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late I Na i) of the cardiac Na v 1.5 channel with improved efficacy and potency relative to ranolazine

Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late I Na i) of the cardiac Na V 1.5 channel with improved efficacy and potency relative to ranolazine

Using Patchxpress to Screen Blockers of the Cardiac Sodium Channel (Nav1.5) for Effects on Late INA, Peak INA, and Channel Kinetics

Partial A(1) adenosine receptor agonists from a molecular perspective and their potential use as chronic ventricular rate control agents during atrial fibrillation (AF)

Affinity and intrinsic efficacy (IE) of 5′-carbamoyl adenosine analogues for the A 1 adenosine receptor—efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Structure–affinity relationships of 5 ′ -aromatic ethers and 5 ′ -aromatic sulfides as partial A 1 adenosine agonists, potential supraventricular anti-arrhythmic agents

CVT-4325: A Potent Fatty Acid Oxidation Inhibitor with Favorable Oral Bioavailability

Structure‐Affinity Relationships of the Affinity of 2‐Pyrazolyl Adenosine Analogues for the Adenosine A 2A Receptor

A1 adenosine receptor agonists and their potential therapeutic applications

A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias

Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi

Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B

The Drug Annotations Series

Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency

Molecule Evoluator CIDRUX BV, Park Oosterspaarn 6, 2036 MB Haarlem, The Netherlands. www. cidrux.com. See Web site for pricing information

Marked difference in saxitoxin and tetrodoxin affinity for the human nociceptive voltage-gated sodium channel (Naᵥ1.7)

A1 adenosine receptor antagonists, agonists, and allosteric enhancers

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