Numerous drug treatments that have recently entered the clinic or clinical trials have their
genesis in zebrafish. Zebrafish are well established for their contribution to developmental …

Pan-Assay Interference Compounds (PAINS) are very familiar to medicinal chemists who
have spent time fruitlessly trying to optimize these nonprogressible compounds. Electronic …

Acetylation of histones by lysine acetyltransferases (KATs) is essential for chromatin
organization and function. Among the genes coding for the MYST family of KATs (KAT5 …

Significant resources in early drug discovery are spent unknowingly pursuing artifacts and
promiscuous bioactive compounds, while understanding the chemical basis for these …

Histone modifications and more specifically ε-lysine acylations are key epigenetic regulators
that control chromatin structure and gene transcription, thereby impacting on various …

KAT6A, and its paralog KAT6B, are histone lysine acetyltransferases (HAT) that acetylate
histone H3K23 and exert an oncogenic role in several tumor types including breast cancer …

It is increasingly clear that academic high-throughput screening (HTS) and virtual HTS triage
suffers from a lack of scientists trained in the art and science of early drug discovery …

Many compounds with potentially reactive chemical motifs and poor physicochemical
properties are published as selective modulators of biomolecules without sufficient …

Enzymes are common targets in high-throughput screening and related campaigns. An
analysis of papers published between 1990 and 2018 showed that kinases were the most …

KAT6A and KAT6B genes are two closely related lysine acetyltransferases that transfer an
acetyl group from acetyl coenzyme A (AcCoA) to lysine residues of target histone substrates …