Development

Question 1

1. Biological Assays

Answer 1

need to be quick, simple, relevant
- in vivo = on life
- in vitro = in glass

Question 2

2. Hit-to-lead

Answer 2

compounds from library shortlisted by:
- synthetic accessibility
-specificity
-toxicity
- physical properties

Question 3

3. Lead optimisation

Answer 3

compounds them optimised for:
- ADME
- toxicity
-physiochem properties (polarity, Ph, Mr)

Question 4

strategies for optimisation

Answer 4

1. adjusting polarity/ charge for mem perm
2. blocking metabolically active sites
3. rigidification

Question 5

Clinical trials

Answer 5

PHASE 1: safety
PHASE 2: efficiacy - small scale
PHASE 3: efficiacy - large scale
PHASE 4: follow up trials