T. M. Willson

Discovery of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach

This paper identifies and characterizes RA-0002034, a covalent inhibitor of CHIKV nsP2 protease, showing potent inhibition and selectivity against alphaviruses.

Synthesis of 5-Benzylamino and 5-Alkylamino-substituted Pyrimidoquinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity

The paper synthesizes pyrimidoquinoline derivatives as CSNK2A inhibitors with antiviral activity, finding that certain substituents improve potency while maintaining solubility.

Discovery and Optimization of Narrow Spectrum Inhibitors of Tousled Like Kinase 2 (TLK2) Using Quantitative Structure Activity Relationships

The paper identifies and optimizes narrow-spectrum TLK2 inhibitors using QSAR analysis and structural studies.

Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3

Optimization of 3-Cyano-7-cyclopropylamino-pyrazolopyrimidines Toward the Development of an In Vivo Chemical Probe for CSNK2

The paper develops analogs of SGC-CK2-1 to improve pharmacokinetic properties in mice by inhibiting GST and P450 enzymes through co-dosing protocols.

Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells

The paper develops a NanoBRET probe to measure PLK1 target engagement in live cells and evaluates its use with known PLK inhibitors.

A new chemotype of chemically tractable nonsteroidal estrogens based on a thienopyrimidine core.

The paper identifies a new chemotype of nonsteroidal estrogens based on a thienopyrimidine core through targeted screening and structure-guided optimization.

Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2

The paper shows that inhibiting the kinase CSNK2 blocks replication of several beta-coronaviruses, including SARS-CoV-2, by preventing viral entry.

Crowdsourced mapping of unexplored target space of kinase inhibitors

The paper benchmarks predictive models for kinase inhibitor potencies using crowdsourced data and identifies new compound-kinase interactions.

The Kinase Chemogenomic Set (KCGS): An open science resource for kinase vulnerability identification

The paper introduces the Kinase Chemogenomic Set (KCGS), a curated collection of 187 selective kinase inhibitors covering 215 human kinases, for use in cell-based screens.

Development of SGC-GAK-1 as an orally active in vivo probe for cyclin G associated kinase through cytochrome P450 inhibition

The paper develops SGC-GAK-1 as an orally active in vivo probe for GAK by using cytochrome P450 inhibition to improve its metabolic stability and plasma exposure.

SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)

The paper describes SGC-GAK-1, a selective GAK inhibitor, and identifies a related compound that inhibits RIPK2 without GAK activity, providing tools to study GAK and RIPK2 biology.

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase

The paper identifies 4-anilinoquinolines as potent GAK inhibitors with high selectivity and suggests their potential as tools for studying GAK's role in infectious diseases.

Progress Towards a Public Chemogenomic Set for Protein Kinases and a Call for Contributions

The paper shares progress on a kinase chemogenomic set, releases inhibitor profiling data, and calls for community collaboration to complete the set.