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Biophysical Assays

Advancements in hit identification for membrane protein drug discovery

Drug Target Review

APRIL 7, 2025

This article explores the potential of fragment-based screening in the GPCR landscape through the lens of the Adenosine A2a receptor, showcasing the development of methods that could help to overcome historical roadblocks in GPCR drug discovery.

Fragment Screening

Fragment Screening Drugs Small Molecule Biophysical Assays

Variability in biological activity measurements reported in the drug discovery literature

Molecular Design

SEPTEMBER 18, 2024

I’ll start by looking at irreversible mechanisms of action and the ( S2017 | McW2021 | H12024 ) articles cover irreversible covalent inhibition (this is the irreversible mechanism of action that ChEMBL users are most likely encounter).

Biochemical Assays

Biochemical Assays Drugs Biophysical Assays Cell Based Assays

Obstacles and innovations of macrocyclic drug development

Drug Target Review

JANUARY 16, 2025

What are macrocycles and why are they interesting for drug discovery? Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 1 However, there has recently been an increased interest in so-called beyond rule-of-five compounds, such as macrocycles.

Drug Development

Drug Development Small Molecule Drugs FDA Approval

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Advancements in hit identification for membrane protein drug discovery

Variability in biological activity measurements reported in the drug discovery literature

Obstacles and innovations of macrocyclic drug development

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