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.
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).
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.
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