Summary DExH-box helicase 9 (DHX9), also known as RNA helicase A (RHA) or nuclear DNA helicase II (NDHII), is rapidly emerging as a high-value target at the intersection of genome stability, innate immunity, and cancer biology. As the first selective DHX9 inhibitors move into preclinical and early clinical development, interest in robust DHX9 inhibitor screening […]
Introduction DNA damage repair (DDR) pathways are essential for maintaining genome stability. When they fail, cancer cells often develop dependencies on backup repair mechanisms—creating therapeutic vulnerabilities. One such pathway, theta-mediated end joining (TMEJ), is orchestrated by DNA polymerase θ (POLQ), a unique enzyme that has become one of the most promising synthetic-lethal targets in oncology. […]
Summary Ultra-high-throughput screening (uHTS) is increasingly the standard in modern drug discovery, enabling the rapid screening of hundreds of thousands to millions of compounds. A key enabler of uHTS is assay miniaturization — shifting formats from 96-well → 384-well → 1536-well plates. While this evolution offers tremendous cost, time, and reagent savings, it also introduces […]
Summary CD38, CD39, and CD73 are extracellular enzymes that regulate adenosine and NAD⁺ signaling in the tumor microenvironment. Robust biochemical assays for these targets quantify substrate turnover—NAD⁺ → ADPR (CD38), ATP/ADP → AMP (CD39), and AMP → Adenosine (CD73)—using sensitive, high-throughput screening (HTS)-ready readouts such as fluorescence polarization (FP), TR-FRET, or fluorescence intensity (FI). For […]
Introduction Drug discovery is increasingly data-driven. Artificial intelligence, machine learning, and automated chemistry have revolutionized how scientists generate and optimize potential therapeutics. But despite the sophistication of these computational tools, they all rely on one essential element: accurate experimental data. That data begins with biochemical assays—the cornerstone of the hit-to-lead (H2L) process. While AI can […]
Summary The VPS4B inhibitor screening assay enables researchers to measure the ATPase activity of VPS4B — a critical enzyme in the endosomal sorting complex required for transport (ESCRT) pathway — to identify small-molecule inhibitors that modulate its function. VPS4B hydrolyzes ATP to power the disassembly of ESCRT-III filaments, a step essential for membrane remodeling, viral […]
Introduction In high-throughput screening (HTS), assay performance determines the success of every downstream discovery step. Whether you’re screening kinase inhibitors, GTPase modulators, or SIRT1 activators, your ability to detect true signal over noise directly affects hit identification and reproducibility. For years, scientists have relied on signal-to-background ratio (S/B) as a quick way to quantify assay […]
Summary (TL;DR) Allosteric inhibitors bind outside an enzyme’s active site and modulate activity by shifting conformations and/or altering catalytic parameters. To find them efficiently, run orthosteric-agnostic primary screens (e.g., product measuring biochemical assays at fixed subsaturating substrate), triage hits with kinetic mapping (substrate titrations to classify competitive vs mixed vs noncompetitive), and confirm allostery with […]
Summary In high-throughput screening (HTS), assay sensitivity directly determines data quality, hit reproducibility, and cost efficiency. High-sensitivity assays detect subtle enzyme activity changes using less enzyme, conserving precious reagents while maintaining accurate kinetic and IC₅₀ measurements—critical for identifying and ranking potent inhibitors. Why Sensitivity Matters in HTS Sensitivity—the ability of an assay to detect minimal […]
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