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Author Details

Jeffrey G Varnes
Oncology R&D
2002
23
13
PMIDPaper TitleJournal TitlePublished Year
36912782Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners.Mol Cancer Ther2023
34570508Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.J Med Chem2021
34647738Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.J Med Chem2021
32988967AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-x<sub>L</sub>, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia.Clin Cancer Res2020
33335676Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.ACS Med Chem Lett2020
33306391Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.J Med Chem2020
32910656Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.J Med Chem2020
31620239Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.ACS Med Chem Lett2019
29266803Structure-Based Design of Selective Noncovalent CDK12 Inhibitors.ChemMedChem2018
29486970Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.Bioorg Med Chem Lett2018
27994749Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.ACS Med Chem Lett2016
26597534Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.Bioorg Med Chem Lett2016
24881567Towards the next generation of dual Bcl-2/Bcl-xL inhibitors.Bioorg Med Chem Lett2014
21295468Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).Bioorg Med Chem Lett2011
21645511Biochemical characterization and in vitro activity of AZ513, a noncovalent, reversible, and noncompetitive inhibitor of fatty acid amide hydrolase.Eur J Pharmacol2011
20637614Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1.Bioorg Med Chem Lett2010
19767451Position 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 evaluation.Mol Pharmacol2009
18054227Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.Bioorg Med Chem Lett2008
17418570CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.Bioorg Med Chem Lett2007
17933529Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.Bioorg Med Chem Lett2007
17315987Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.J Med Chem2007
15026042Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.Bioorg Med Chem Lett2004
12067561CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.Bioorg Med Chem Lett2002
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Collaborators

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School of Clinical Sciences at Monash Health, Monash University
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Wellcome Sanger Institute
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Repare Therapeutics Inc.
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Oregon Health & Science University, University of California Berkeley
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