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Sign up for email updates!Part 2: Free Drug Principle and Potency
Often times free fraction corrected potency values are not reported in the literature. However, protein or matrix binding can have drastic effects on potencies and should be considered when interpreting data. This article discusses why correcting potencies with free fraction measurements is important.
Patent Busting: Move a nitrogen, file a patent
Casma Therapeutics recently disclosed a patent application focused on TRPML1 agonists, a lysosomal ion channel involved in lysosomal storage diseases. Their patent application is an iteration from prior art by Caraway Therapeutics (now Merck) where they moved one nitrogen on the molecules' core.
Identifying small molecule RNA binders using covalent tethering
A publication from the Disney Lab at UF Scripps Institute identifies a new mustard-like RNA reactive electrophile and applies covalent fragment-based screening to identify small molecule RNA binders. Could this approach be used more broadly to discover non-covalent RNA and protein binders?
Maze stock increases 55% in one day after reporting favorable phase 1 data for MZE782 and private investment of $150 million
Maze Therapeutics focuses on treating kidney disorders with two clinical assets. Maze reported yesterday favorable phase 1 data for MZE782, a small molecule inhibitor of a neutral amino acid transporter, SLC6A19.
Putting the free drug principle into practice to calculate brain penetrance and other PK/PD parameters
The free drug hypothesis principle is often ignored in publications. This article is a crash course on how to
apply the free drug principle to calculate free (unbound) concentrations to correct for non-specific protein binding. I swear it is easy and requires
very limited math!
Violet therapeutics are targeting EphB3 for neurodegenerative diseases including Alzheimer's
Violet Therapeutics is a platform biotech company that identified EphB3 as a cell receptor involved in neuroinflammation. This article discusses their development of covalent small molecule inhibitors of EphB3.
Part 3: Patent Busting A Literature-based Approach
Part 3 of the patent busting Literature-based Approach series focuses on
identifying GAPS in a patent focused on
STING antagonists and discusses how to differentiate to design novel chemical matter.
Vinyl sulfonimidamides as a new cysteine reactive electrophile
Sanofi completes buyout of Vigil Neurosciences for a small molecule TREM2 agonist program
ChemUI Seek: Download this cool chemical structure search application
Part 2: The case for CD47-SIRPα small molecule inhibition
The case for CD47-SIRPα small molecule inhibition
The other day I was perusing Arch Venture’s company portfolio and landed on...
Orthosteric versus allosteric SARM1 inhibitors
APOE4 increases inflammation related pathways
Patent Busting A Literature-based Approach
Part 2: Patent Busting A Literature-based Approach
My First Article! Allow me to introduce myself
Welcome to my first ever blog post! I know the name ChemJam might seem like a terrible choice to many people, but the domain name was supremely cheap, and I currently don’t have a consistent income right now (Hire me!). So, you will just have to deal with it...