Lead Discovery and Optimization Framework
Assay
Development
Target(s)
Scalability
Off Target Activity
Screen
Development
Readout
Scalability
Sample Testing
Screening
Scale up (HTS)
Automation
Data Management
Lead
Identification
Pharmacokinetics Toxicity
Info. Management
Lead
Optimization
Med. Chemistry
Toxicity
info. Management
Strategic Decisions
Governance Management
Novelty
Enhanced Activity
Hit Rate
Controls
Reproducibility
Hit Identification
Literature
Patentability
Compound
Management
Iterative Discover and Optimization
Lead Discovery and Optimization Delivery Methodology
Establish (Plan)
Implement and Operation (Do)
Monitor and Review (Check)
Maintain and Improve (Act)
Plan Phase
- Evaluate market opportunities
- Define target(s) and molecule class
- Establish proof of concept (POC)
- Assay
- Readout
- Develop screening strategy
Do Phase
- Perform POC
- Implement strategies for screening
- Scalability
- Metrics
- Hit Selection
- Lead selection
- Lead optimization
Check Phase
- Critical path
- Toxicity
- Mode of action
- Off-target activity
- Medicinal Chemistry
- Lead optimization
- Project Team review
Act Phase
- Management adjusts program as per market opportunity
- Management reviews program (go/ no go)