Fragment-to-lead
Fragment-To-Lead
A strategy for identifying target-specific leads by screening libraries composed of small, low molecular weight molecules and subject them to cycles of synthetic elaborations.
Our FBDD approach will be presented by our partner György M Keserű, research professor, RCNS Hungary, at the EFMC International Symposium on Medicinal Chemistry.
Find a description of our approach in our newly published white paper:
“Lead Discovery for Hot Spots – FBDD by Smart Fragment Libraries and Expanded Chemical Space”
To view the full publication in Nature Communications entitled Exploring protein hotspots by optimized fragment pharmacophores - Associated Paper from Nature Communications
To learn more - Summary in Chemistry Community
Case Study A: Discovery to Preclinical Development
- Served as a customized chemistry department for a small biotech
- Difficult target and assay
- Leads substantially improved over hits despite long SAR cycles
- Program sold to Pharma
Case Study B: Screening Hits to Patented Leads
- Served as the chemistry department for a virtual biotech
- Patents issued in congested IP space
- Program sold to Pharma
Case Study D: Early Lead to Clinical Candidate
- Served as a complimentary chemistry team for a medium sized biotech
- Improved pharmaceutical properties allowed in vivo activity
- Program met external milestone