This section contains case studies, industry highlights, minireviews, and other articles for drug discovery professionals. Check out the resources page for posters, educational content, lists of drug approvals, and more.
The Merck bicyclic macrocyclic peptide PCSK9 inhibitor, “compound 44,” is a highly potent (Ki = 0.00239 nM) and orally bioavailable…
molecule
1 year ago ●
1 min read
The Janssen non-ATP competitive HPK1 inhibitor, “compound 1,” was identified from a screening cascade specifically looking for allosteric inhibitors, which…
molecule
1 year ago ●
1 min read
The Entasis broad-spectrum antibiotic, ETX0462, is both an inhibitor of penicillin-binding proteins (PBPs, the target of beta-lactams) and a beta-lactamase inhibitor…
molecule
1 year ago ●
3 mins read
The BMS factor XIa inhibitor, milvexian (BMS-986177), is an oral antithrombotic with a Ki of 0.11 nM. A member of this macrocyclic…
molecule
1 year ago ●
1 min read
The GSK DNMT1 inhibitor GSK3685032 is a first-in-class, non-nucleoside, reversible and selective inhibitor of the epigenetic target DNA-methyltransferase 1 (DNMT1). Commonly prescribed…
molecule
1 year ago ●
1 min read
The Janssen PRMT5 inhibitor, onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with high selectivity…
molecule
1 year ago ●
1 min read
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