6 Questions
What is the main issue with the innovation deficit of new chemical entities?
Difficulty in validating hit compounds
Why is the drug discovery process often referred to as a wasteful game?
Due to the high cost of drug development
What is drugability in the context of drug design?
The ability of a compound to bind to a drug target
How do hit compounds differ from lead compounds in the drug discovery process?
Hit compounds have lower binding affinity than lead compounds
What technique is currently used for testing the validated hit or lead compounds?
High-throughput screening
What criteria must a hit fulfill to be accepted as a lead compound in drug design?
High binding affinity and low selectivity
Study Notes
Innovation Deficit of New Chemical Entities
- The main issue is the decline in the number of new medicines being approved despite increasing R&D investments.
Drug Discovery Process
- The process is often referred to as a wasteful game due to the high failure rate of candidate compounds, with up to 90% of them failing to reach the market.
Drugability
- In drug design, drugability refers to the likelihood of a biological target being modulated by a small molecule.
Hit Compounds vs Lead Compounds
- Hit compounds are molecules that show preliminary activity against a target, while lead compounds are optimized hit compounds that have been validated through further testing.
- Lead compounds are chosen based on their potency, selectivity, and pharmacokinetic properties.
Testing Validated Compounds
- Currently, biochemical assays, cell-based assays, and animal models are used for testing validated hit or lead compounds.
Hit to Lead Criteria
- A hit must fulfill certain criteria to be accepted as a lead compound, including:
- Sufficient potency and selectivity
- Favorable pharmacokinetic properties
- Low toxicity and good safety profile
- Ability to be formulated and delivered effectively
Test your knowledge of drug design with these study aids questions. This quiz provides a summary of the drug design submodule, allowing you to assess and enhance your understanding of the topic.
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