Hit-to-Lead Archives - Page 2 of 9

Covalent Fragment-based Drug Discovery: BTK Inhibitors

At the Covalent Drug Discovery 2023 Summit and Fragments 2024 Conference, we presented a case study on Bruton’s tyrosine kinase (BTK)...

One Stop Target-to-Hit Platform: CDKs and CDK-Cyclin Complexes

Cyclin-dependent kinases (CDKs) and their cyclin regulatory subunits form complexes that are essential for driving abnormal growth processes in cancer...

Biophysical and Structural Biology Methods Enable Fragment-Based Ligand Discovery

Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in...

Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor

DNA-dependent protein kinase (DNA-PK) plays an important role in the overall survival and proliferation of cells, making this enzyme an...

OncoWuXi Express: Large-scale Cell Panel Screening Platform for Integrated Pharmacogenomics and Bioinformatics Research

Introduction: OncoWuXi Express will continue to keep you informed about updates to our on-line tumor model database (OncoWuXi Database), as...

Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug...

Dianthus Platform: Screening for Modulators of SIK3

Salt-inducible kinases (SIKs) have recently emerged as key regulators of oncogenesis, inflammation, and immune responses, making these enzymes an important...

Dianthus Platform: Screening for CRBN-DDB1 Proteolysis-Targeting Chimeras and Molecular Glues

Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of...

Dianthus Platform: Screening for Inhibitors of PIK3CA-PIK3R1

Within the PI3K family, the heterodimer comprising the p110-α catalytic and p85-α regulatory subunits (encoded by PIK3CA and PIK3R1) is...

Knowledge Library