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Publications

Discovery and Development Strategies for SARS-CoV-2 NSP3 Macrodomain Inhibitors

Schuller M. et al, (2023), Pathogens, 12, 324 - 324

Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.

Londregan AT. et al, (2023), Journal of medicinal chemistry, 66, 460 - 472

Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.

Serafim RAM. et al, (2021), Journal of medicinal chemistry

Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.

Henderson SH. et al, (2021), Journal of medicinal chemistry, 64, 11709 - 11728

Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain

Brand M. et al, (2021), Journal of Medicinal Chemistry

Fragment Binding to the Nsp3 Macrodomain of SARS-CoV-2 Identified Through Crystallographic Screening and Computational Docking.

Schuller M. et al, (2020), bioRxiv

Open Science Discovery of Potent Non-Covalent SARS-CoV-2 Main Protease Inhibitors

Achdout H. et al, (2020)

DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity

Schröder M. et al, (2020), Journal of Medicinal Chemistry, 63, 10224 - 10234

Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor

Hassell-Hart S. et al, (2020), ORGANOMETALLICS, 39, 408 - 416

Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1

Ni X. et al, (2019), ACS Medicinal Chemistry Letters, 10, 1661 - 1666

A chemical toolbox for the study of bromodomains and epigenetic signaling

Wu Q. et al, (2019), Nature Communications, 10

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function

Fagan V. et al, (2019), Journal of Medicinal Chemistry, 62, 9008 - 9025

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1)

Xiong Y. et al, (2019), Journal of Medicinal Chemistry, 62, 8996 - 9007

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Le Bihan Y-V. et al, (2019), European Journal of Medicinal Chemistry, 177, 316 - 337

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening

Resnick E. et al, (2019), Journal of the American Chemical Society, 141, 8951 - 8968

A Chemical Probe For Tudor Domain Protein Spindlin1 to Investigate Chromatin Functions

Fagan V. et al, (2019)

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).

Asquith CRM. et al, (2019), Journal of medicinal chemistry, 62, 2830 - 2836

Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.

Christott T. et al, (2019), SLAS Discov, 24, 133 - 141

An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

D'Ascenzio M. et al, (2019), Angewandte Chemie International Edition, 58, 1007 - 1012

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

Vazquez‐Rodriguez S. et al, (2019), Angewandte Chemie International Edition, 58, 515 - 519

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