Protein kinases are highly tractable targets for drug discovery. However, the biological
function and therapeutic potential of the majority of the 500+ human protein kinases remains …

Building on the pyrazolopyrimidine CK2 (casein kinase 2) inhibitor scaffold, we designed a
small targeted library. Through comprehensive evaluation of inhibitor selectivity, we identified …

We describe the assembly and annotation of a chemogenomic set of protein kinase inhibitors
as an open science resource for studying kinase biology. The set only includes inhibitors …

β-Catenin-dependent WNT signal transduction governs development, tissue homeostasis,
and a vast array of human diseases. Signal propagation through a WNT-Frizzled/LRP …

The Tribbles family of pseudokinases recruits substrates to the ubiquitin ligase COP1 to facilitate
ubiquitylation. CCAAT/enhancer-binding protein (C/EBP) family transcription factors are …

This important study reports selective CDKL5 inhibitors that may be of high interest to
investigate the role of this kinase in disease (particularly, in CDKL5 deficiency disorder) and to …

Tau tubulin kinase 1 and 2 (TTBK1/2) are highly homologous kinases that are expressed
and mediate disease-relevant pathways predominantly in the brain. Distinct roles for TTBK1 …

Inhibition of the protein kinase CSNK2 with any of 30 specific and selective inhibitors
representing different chemotypes, blocked replication of pathogenic human, bat, and murine β-…

3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines, including the chemical probe SGC-CK2-1,
are potent and selective inhibitors of CSNK2A in cells but have limited utility in …

Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual
AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC-AAK1-1…