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Modifications at the 3 position of the pyridine ring led to a number of potent compounds with improved physical properties, resulting in the identification of 11g as a promising, orally active Akt inhibitor.
In order for medicinal chemists to tune solubility of lead compounds, a rapid assay is needed to provide solubility data that is accurate and predictive so that it can be reliably used for designing the next generation of compounds with improved properties.
There is a growing scientific interest in the influence of photocatalysis on synthesis of compounds with improved properties.
We therefore identified an opportunity to create a facile discovery platform enabling the characterization of existing DOT1L inhibitors, and the preparation of new compounds with improved properties.
This step calls for a fast, flexible, and cost-effective strategies to meet the demands of producing arrays of high-content lead compounds with improved efficiency for better clinical success.
This highlights the need to search for novel agents such as fatty acid compounds with improved potency against seizures and a better side-effects profile compared with the drugs currently available.
This resulted in compounds with improved CYP 3A4 profiles.
Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro.
Clearances in vitro and in vivo were monitored to identify compounds with improved plasma stability.
Our efforts resulted in new compounds with improved binding affinity and selectivity.
New potent and selective lead compounds with improved metabolic properties were identified.
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CEO of Professional Science Editing for Scientists @ prosciediting.com