Lead Optimization
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
