C. I. Wells

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.

A Potent and Selective CDKL5/GSK3 Chemical Probe is Neuroprotective

The paper develops a potent and selective CDKL5/GSK3 chemical probe and demonstrates its neuroprotective effects in human motor neurons under ER stress.

SGC-CAMKK2-1: A chemical probe for CAMKK2

This paper introduces SGC-CAMKK2-1, a selective chemical probe for CAMKK2, demonstrating its potential as a tool to study the therapeutic benefits of CAMKK2 inhibition.

SGC-CLK-1 (CAF-170) a chemical probe for the Cdc2-Like kinases CLK1, CLK2, and CLK4

This paper identifies and characterizes SGC-CLK-1, a potent inhibitor of CLK1, CLK2, and CLK4, showing its selectivity and effects on SR protein phosphorylation and localization.

An open source plant kinase chemogenomics set

The paper presents a plant kinase chemogenomics set, identifying compounds that affect root development in Arabidopsis and rice, with implications for understanding plant kinase function.

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.

Temozolomide-induced guanine mutations create exploitable vulnerabilities of guanine-rich DNA and RNA regions in drug resistant gliomas

This study identifies guanine mutations in TMZ-resistant gliomas that disrupt G4 structures and splice sites, creating vulnerabilities targeted by G4 stabilizers and splicing inhibitors.

Non-canonical role of Hippo tumor suppressor serine/threonine kinase 3 STK3 in prostate cancer

This study shows that STK3, typically a tumor suppressor, promotes prostate cancer growth and identifies STK3 inhibitors with therapeutic potential.

Targeting the water network in cyclin G associated kinase (GAK) with 4-anilino-quin(az)oline inhibitors

This paper designs and tests 4-anilinoquinoline inhibitors targeting cyclin G-associated kinase (GAK) by analyzing water networks in the ATP binding site.

Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3)

The paper identifies 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine as a potent PKN3 inhibitor with an IC50 of 1.3 μM in cells, suggesting its potential as a tool for studying PKN3 biology and therapeutic applications.

In depth analysis of kinase cross screening data to identify CAMKK2 inhibitory scaffolds

This paper reviews CAMKK2's role in biology and disease, identifies starting points for inhibitor development using literature and databases, and highlights potential for selective inhibitors in oncology, metabolism, and inflammation.

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.

Design and analysis of the 4-anilino-quin(az)oline kinase inhibition profiles of GAK/SLK/STK10 using quantitative structure activity relationships

The paper designs and synthesizes 4-anilino-quin(az)oline compounds to analyze their kinase inhibition profiles and structure-activity relationships for GAK/SLK/STK10 targets.

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.

Identification of Kinase Inhibitors that Regulate Nuclear Receptor Nurr1 (NR4A2) Cellular Activity

The paper identifies kinase inhibitors that modulate Nurr1 (NR4A2) cellular activity by developing a luciferase-based assay and screening a kinase inhibitor set.

Cyclin F-Chk1 synthetic lethality mediated by E2F1 degradation

The paper identifies synthetic lethality between Chk1 inhibition and cyclin F loss, revealing Cyclin F's role in preventing DNA replication stress via E2F1 degradation.

Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

The paper designs a set of GAK/EGFR inhibitors to study their relationship in chordoma and characterizes their activity in vitro and through target engagement assays.

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.

In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases

The paper analyzes kinase cross-screening data to identify potential chemical starting points for inhibiting Nek kinases, aiming to advance drug discovery for these understudied targets.

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations

The paper identifies BI-D1870 as a starting point for VRK inhibitors and reports co-crystal structures revealing different P-loop conformations in VRK1 and VRK2.

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.