Lead Optimization

January 14, 2025

Identification of TLR7 Antagonists with Novel Scaffold

Hit optimization through fast SAR exploration

Background

•Toll-like receptors (TLRs) are a family of pattern recognition receptors critical to the innate immune system. Dysregulated activation of TLR7/8 has been linked to the progression of autoimmune diseases, such as Systemic Lupus Erythematosus (SLE).

•The hit compounds identified through virtual screening feature a completely novel scaffold with superior micromolar activiy against TLR7, holding promise for further optimization to enhance their potency.

Hit Optimization Workflow
Results