Contemporary Drug Discovery

Annotations:

• So we can identify The target Sites 

1. Modern

   Annotations:

   • Genome analysis Gene regulation Proteomics
   1. Proteomics

      Annotations:

      • Drug structure determination based on protein structure
2. Traditional

   Annotations:

   • -Long winded -examine effect of natural compounds on varying tissues -differing effects mean differing locks
3. Target Validation

   Annotations:

   • The target must be vital to the disease so that when we inhibit it it modifies the disease in some way. 
   1. Competator clash?
   2. Novel compound risks?

1. Natural compunds
2. Copycat leads
3. Chance disoveries
4. High Throughput screening
5. Chemical libraries
6. Virtual screening
7. WHat makes a good lead?
   1. Is it synthetically tractble?
   2. Is it a good root to diversify ?
   3. Physiochemical properties we should know?

1. Can we trust literature derived compounds?
2. reasons for failiure
   1. Lipinkski's rule of five

      Annotations:

      • This rule of thumb is a rudementary method for measuring the bioavailability of the compounds.
   2. poor PK
   3. Poor Solubility