article thumbnail

Biochemical and Structural Studies of Protein Tyrosine Phosphatase PTP‐PEST (PTPN12) in Search of Small Molecule Inhibitors

Chemical Biology and Drug Design

The invitro biochemical assays validated that J1-65 inhibits PTP-PEST activity competitively and the inhibitor binding stabilizes the protein-ligand complex. An in-house molecule library was screened using in silico molecular docking, and a myo-inositol derivative was identified as a potent hit molecule.

article thumbnail

Assembling data sets for training ML bioactivity models

Molecular Design

If this seems a bit extreme it’s worth pointing out that to accurately measure an IC 50 value of 10 μM requires that the compound be soluble, while neither aggregating nor interfering with assay read-out, at a concentration of 100 μM.

Insiders

Sign Up for our Newsletter

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

article thumbnail

High Throughput Screening (HTS)

Sygnature Discovery

Advanced Automation in Sygnature Discoverys HTS System Our high throughput screening system, developed by HighRes Biosolutions, is designed for versatility, accommodating both cell and biochemical assays. Central to our automation is the Echo acoustic dispensing technology, ensuring highly accurate compound delivery.

article thumbnail

#WhyIScienceQ&A: A neuroscientist advocates for stepping outside your comfort zone in research

Broad Institute

Today, she uses induced pluripotent stem (iPS) cells, mouse models, biochemical assays, and high-throughput screening to study the role of TMED cargo receptors in Alzheimer’s disease. I love the idea of studying biology at its core, where the same basic principles can apply across different systems.”

article thumbnail

Biochemical assays and deep cyclic inhibition in cancer treatment

Drug Target Review

Molecular-level biochemical assays like transcriptomics, genomics and proteomics have emerged as valuable tools for identifying potential targets in cancer treatment through deep cyclic inhibition (DCI).

article thumbnail

Structural Dynamics of the Ubiquitin Specific Protease USP30 in Complex with a Cyanopyrrolidine-Containing Covalent Inhibitor

Covalent Modifiers

We have integrated structural and quantitative proteomics with biochemical assays to decipher the mode of action of covalent USP30 inhibition by a small molecule containing a cyanopyrrolidine reactive group, USP30-I-1. The inhibitor demonstrated high potency and selectivity for endogenous USP30 in neuroblastoma cells.

article thumbnail

Positive Impact of Dragonfly™ Discovery in Biochemical Assay

Zobio

Biochemical assays are commonly used to assess how organic compounds impact the activity of a protein of interest (POI). Het bericht Positive Impact of Dragonfly™ Discovery in Biochemical Assay verscheen eerst op ZoBio - Drug Discovery Technology.