GO - Lead Activity Compounds

Question 1

Lead discovery is

Answer 1

when you find new chemical entities which by subsequent modification may be transformed into a clinically useful drug

Question 2

Lead generation is

Answer 2

when you find compounds which possess a desired but non-optimised biological activity.

Question 3

Lead activity molecules are not automatically good molecules because they may

Answer 3

• be peptidic (many venoms and hormones); poorly absorbed, rapidly cleared due to enzymatic degradation or rapidly cleared due to renal clearance.
• have poor ‘drug-like’ properties; poor pharmakinetic profile

Question 4

What are the four strategies for the discovery of lead activity molecules?

Answer 4

• systematic screening
• planned research and rational drug design
• improving existing drugs
• exploiting biological information
• often a combination of these