Robert J. Sheppard

AstraZeneca (Brazil) — Brazil

Biochemistry, Genetics and Molecular Biology · Life Sciences

20h-index2.7kcitations33works0.02yr avg
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Research Topics

Protein Degradation and Inhibitors(10), Ubiquitin and proteasome pathways(7), RNA and protein synthesis mechanisms(5), Multiple Myeloma Research and Treatments(5), Chemical Synthesis and Analysis(5)

Publications33 total

Solvent Sustainability in Drug Discovery: Where Are We Now, and How Can We Improve?
Journal of Medicinal Chemistry·2025Open Access
Biocatalysis in Drug Design: Engineered Reductive Aminases (RedAms) Are Used to Access Chiral Building Blocks with Multiple Stereocenters
Journal of the American Chemical Society·2023· 12 citedOpen Access
Drug discovery for epigenetics targets
Drug Discovery Today·2021· 31 cited
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode
Journal of Medicinal Chemistry·2020· 22 citedOpen Access
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification
Journal of Medicinal Chemistry·2019· 34 citedOpen Access
Route to Prolonged Residence Time at the Histamine H <sub>1</sub> Receptor: Growing from Desloratadine to Rupatadine
Journal of Medicinal Chemistry·2019· 20 citedOpen Access
Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor
Scientific Reports·2019· 24 citedOpen Access
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors
Journal of Medicinal Chemistry·2018· 26 citedOpen Access
Structure–Affinity Relationships and Structure–Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists
Journal of Medicinal Chemistry·2017· 9 citedOpen Access
Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics
Molecular Pharmacology·2016· 25 citedOpen Access
A Chemical Probe for the ATAD2 Bromodomain
Angewandte Chemie International Edition·2016· 75 citedOpen Access
A Chemical Probe for the ATAD2 Bromodomain
Angewandte Chemie·2016· 13 cited
Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics
ACS Chemical Biology·2016· 42 cited
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
ACS Medicinal Chemistry Letters·2016· 64 citedOpen Access
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives
Journal of Medicinal Chemistry·2016· 59 citedOpen Access
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors
Journal of Medicinal Chemistry·2015· 83 citedOpen Access
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
Journal of Medicinal Chemistry·2015· 79 citedOpen Access
Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation
Nature Chemical Biology·2015· 720 citedOpen Access
Kruidenier et al. reply
Nature·2014· 19 citedOpen Access
ChemInform Abstract: [2,3]‐Sigmatropic Rearrangement of Allylic Selenimides: Strategy for the Synthesis of Peptides, Peptidomimetics, and N‐Aryl Vinyl Glycines.
ChemInform·2014
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Frequent Co-authors

Chun‐wa Chung(13), Rab K. Prinjha(12), Emmanuel H. Demont(9), Paul Bamborough(9), Darren J. Mitchell(9), Robert J. Watson(9), Hawa Diallo(8), Paola Grandi(8), Anne‐Marie Michon(8), Emma J. Jones(7), Rebecca C. Furze(6), Gérard Joberty(5), Gerard Drewes(5), David M. Wilson(5), Peter D. Craggs(5), Richard L. Jarvest(5), Andrew K. Forrest(5), Peter J. O’Hanlon(5), Clement Douault(5), Christina Rau(5)