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The pKBHX Database: Toward a Better Understanding of Hydrogen-Bond Basicity for Medicinal Chemists

Journal of medicinal chemistry, 2009-07, Vol.52 (14), p.4073-4086

2009

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The Proteome‐Wide Potential for Reversible Covalency at Cysteine

Angewandte Chemie International Edition, 2019-08, Vol.58 (33), p.11385-11389

International ed. in English, 2019

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Discovery of Reversible Covalent Bruton’s Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib)

Journal of medicinal chemistry, 2022-04, Vol.65 (7), p.5300-5316

2022

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Small Molecule Conformational Preferences Derived from Crystal Structure Data. A Medicinal Chemistry Focused Analysis

Journal of chemical information and modeling, 2008-01, Vol.48 (1), p.1-24

2008

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The pK(BHX) database: toward a better understanding of hydrogen-bond basicity for medicinal chemists

Journal of medicinal chemistry, 2009-07, Vol.52 (14), p.4073-4086

2009

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Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease

The Journal of immunology (1950), 2021-04, Vol.206 (7), p.1454-1468

2021

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Prolonged and tunable residence time using reversible covalent kinase inhibitors

Nature chemical biology, 2015-07, Vol.11 (7), p.525-531

2015

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Discovery of the Irreversible Covalent FGFR Inhibitor 8‑(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3‑d]pyrimidin-7(8H)‑one (PRN1371) for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2017-08, Vol.60 (15), p.6516-6527

2017

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Targeting Interleukin-2-inducible T-cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694

The Journal of biological chemistry, 2015-03, Vol.290 (10), p.5960-5978

2015

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The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance

Molecular cancer therapeutics, 2017-12, Vol.16 (12), p.2668-2676

2017

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The role of enzyme distortion in the single displacement mechanism of family 19 chitinases

Proceedings of the National Academy of Sciences - PNAS, 1998-04, Vol.95 (8), p.4276-4281

1998

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Discovery of a Novel Series of Potent Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B

Journal of medicinal chemistry, 2013-10, Vol.56 (20), p.8163-8182

2013

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De Novo Fragment Design: A Medicinal Chemistry Approach to Fragment-Based Lead Generation

Journal of medicinal chemistry, 2013-04, Vol.56 (7), p.3115-3119

2013

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Quinolones as HCV NS5B polymerase inhibitors

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.82-87

2011

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3-Heterocyclyl quinolone inhibitors of the HCV NS5B polymerase

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.300-304

2012

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The Proteome‐Wide Potential for Reversible Covalency at Cysteine

Angewandte Chemie, 2019-08, Vol.131 (33), p.11507-11511

2019

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Abstract SY30-01: Discovery of the highly selective covalent FGFR1-4 inhibitor PRN1371, currently in development for the treatment of solid tumors

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.SY30-01-SY30-01

Brameld, Ken A.

2016

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Substrate Distortion to a Boat Conformation at Subsite −1 Is Critical in the Mechanism of Family 18 Chitinases

Journal of the American Chemical Society, 1998-04, Vol.120 (15), p.3571-3580

1998

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Ab Initio Quantum Mechanical Study of the Structures and Energies for the Pseudorotation of 5‘-Dehydroxy Analogues of 2‘-Deoxyribose and Ribose Sugars

Journal of the American Chemical Society, 1999-02, Vol.121 (5), p.985-993

1999

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Conformational analysis of aqueous pullulan oligomers: an effective computational approach

Polymer (Guilford), 2002, Vol.43 (2), p.509-516

2002

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Abstract 2091: PRN1371, an irreversible, covalent inhibitor of FGFR1-4 exhibits sustained pathway inhibition in cancer cell lines

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.2091-2091

2017

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Abstract 1249: PRN1371, an irreversible, covalent inhibitor of FGFR1, 2, 3 and 4 is highly efficacious in preclinical tumor models

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.1249-1249

2016

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Substrate assistance in the mechanism of family 18 chitinases: theoretical studies of potential intermediates and inhibitors 1 1Edited by B. Honig

Journal of molecular biology, 1998-07, Vol.280 (5), p.913-923

1998

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The pK BHX Database: Toward a Better Understanding of Hydrogen-Bond Basicity for Medicinal Chemists

Journal of medicinal chemistry, 2009-07, Vol.52 (14), p.4073-4086

2009

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The pKBHX Database: Toward a Better Understanding of Hydrogen-Bond Basicity for Medicinal Chemists

The Proteome‐Wide Potential for Reversible Covalency at Cysteine

Discovery of Reversible Covalent Bruton’s Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib)

Small Molecule Conformational Preferences Derived from Crystal Structure Data. A Medicinal Chemistry Focused Analysis

The pK(BHX) database: toward a better understanding of hydrogen-bond basicity for medicinal chemists

Discovery of N‑[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo‑1H‑pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase

Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease

Prolonged and tunable residence time using reversible covalent kinase inhibitors

Discovery of the Irreversible Covalent FGFR Inhibitor 8‑(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3‑d]pyrimidin-7(8H)‑one (PRN1371) for the Treatment of Solid Tumors

Targeting Interleukin-2-inducible T-cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694

The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance

The role of enzyme distortion in the single displacement mechanism of family 19 chitinases

Discovery of a Novel Series of Potent Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B

De Novo Fragment Design: A Medicinal Chemistry Approach to Fragment-Based Lead Generation

Quinolones as HCV NS5B polymerase inhibitors

3-Heterocyclyl quinolone inhibitors of the HCV NS5B polymerase

The Proteome‐Wide Potential for Reversible Covalency at Cysteine

Abstract SY30-01: Discovery of the highly selective covalent FGFR1-4 inhibitor PRN1371, currently in development for the treatment of solid tumors

Substrate Distortion to a Boat Conformation at Subsite −1 Is Critical in the Mechanism of Family 18 Chitinases

Ab Initio Quantum Mechanical Study of the Structures and Energies for the Pseudorotation of 5‘-Dehydroxy Analogues of 2‘-Deoxyribose and Ribose Sugars

Conformational analysis of aqueous pullulan oligomers: an effective computational approach

Abstract 2091: PRN1371, an irreversible, covalent inhibitor of FGFR1-4 exhibits sustained pathway inhibition in cancer cell lines

Abstract 1249: PRN1371, an irreversible, covalent inhibitor of FGFR1, 2, 3 and 4 is highly efficacious in preclinical tumor models

Substrate assistance in the mechanism of family 18 chitinases: theoretical studies of potential intermediates and inhibitors 1 1Edited by B. Honig

The pK BHX Database: Toward a Better Understanding of Hydrogen-Bond Basicity for Medicinal Chemists

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