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DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors

Journal of medicinal chemistry, 2020-04, Vol.63 (7), p.3552-3562

2020

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The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors

ACS medicinal chemistry letters, 2021-11, Vol.12 (11), p.1649-1655

2021

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The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor

Molecular pharmacology, 2005-04, Vol.67 (4), p.1268-1282

2005

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GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage

Journal of medicinal chemistry, 2020-04, Vol.63 (8), p.4155-4170

2020

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Novel Spiroketal Pyrrolidine GSK2336805 Potently Inhibits Key Hepatitis C Virus Genotype 1b Mutants: From Lead to Clinical Compound

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.2058-2073

2014

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Antiviral Drugs: From Basic Discovery Through Clinical Trials

Kazmierski, Wieslaw M

1, 2011

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Pharmacological disruption of hepatitis C NS5A protein intra- and intermolecular conformations

Journal of general virology, 2014-02, Vol.95 (Pt 2), p.363-372

2014

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Peptide and Protein Design for Biopharmaceutical Applications

Journal of medicinal chemistry, 2010-07, Vol.53 (13), p.5059-5059

Kazmierski, Wieslaw M

2010

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Preclinical Characterization of GSK2336805, a Novel Inhibitor of Hepatitis C Virus Replication That Selects for Resistance in NS5A

Antimicrobial Agents and Chemotherapy, 2014-01, Vol.58 (1), p.38-47

2014

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The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

Molecular pharmacology, 2009-03, Vol.75 (3), p.490-501

2009

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Discovery of Novel Urea-Based Hepatitis C Protease Inhibitors with High Potency against Protease-Inhibitor-Resistant Mutants

Journal of medicinal chemistry, 2012-04, Vol.55 (7), p.3021-3026

2012

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Biological and Structural Characterization of Rotamers of C–C Chemokine Receptor Type 5 (CCR5) Inhibitor GSK214096

ACS medicinal chemistry letters, 2014-12, Vol.5 (12), p.1296-1299

2014

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Novel 4,4-Disubstituted Piperidine-Based C–C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile

Journal of medicinal chemistry, 2011-06, Vol.54 (11), p.3756-3767

2011

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Discovery of a novel series of cyclic urea as potent CCR5 antagonists

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6381-6385

2011

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Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (24), p.7317-7322

2010

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Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties

Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (7), p.2048-2054

2011

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Discovery of next generation inhibitors of HIV protease

Current topics in medicinal chemistry, 2005-12, Vol.5 (16), p.1589-1607

2005

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Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors

Bioorganic & medicinal chemistry, 2003-07, Vol.11 (13), p.2663-2676

2003

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Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease

Bioorganic & medicinal chemistry letters, 2010-06, Vol.20 (12), p.3550-3556

2010

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Discovery of N-benzyl- N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): Optimization of the amine portion

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (24), p.7397-7400

2010

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A new type of synthetic peptide library for identifying ligand-binding activity

Nature (London), 1991-11, Vol.354 (6348), p.82-84

1991

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Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6470-6475

2011

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Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties

Bioorganic & medicinal chemistry letters, 2004-11, Vol.14 (22), p.5689-5692

2004

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Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the Human Immunodeficiency Virus-1

Journal of medicinal chemistry, 2008-10, Vol.51 (20), p.6538-6546

2008

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[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists : derivatizations at the N-terminal of the piperidine ring

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (6), p.1610-1613

2009

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DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors

The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors

The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor

GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage

Novel Spiroketal Pyrrolidine GSK2336805 Potently Inhibits Key Hepatitis C Virus Genotype 1b Mutants: From Lead to Clinical Compound

Antiviral Drugs: From Basic Discovery Through Clinical Trials

Pharmacological disruption of hepatitis C NS5A protein intra- and intermolecular conformations

Peptide and Protein Design for Biopharmaceutical Applications

Preclinical Characterization of GSK2336805, a Novel Inhibitor of Hepatitis C Virus Replication That Selects for Resistance in NS5A

The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

Discovery of Novel Urea-Based Hepatitis C Protease Inhibitors with High Potency against Protease-Inhibitor-Resistant Mutants

Biological and Structural Characterization of Rotamers of C–C Chemokine Receptor Type 5 (CCR5) Inhibitor GSK214096

Novel 4,4-Disubstituted Piperidine-Based C–C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile

Discovery of a novel series of cyclic urea as potent CCR5 antagonists

Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease

Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties

Discovery of next generation inhibitors of HIV protease

Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors

Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease

Discovery of N-benzyl- N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): Optimization of the amine portion

A new type of synthetic peptide library for identifying ligand-binding activity

Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats

Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties

Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the Human Immunodeficiency Virus-1

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists : derivatizations at the N-terminal of the piperidine ring

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