Lead optimisation

Question 1

what are the core concepts of small molecule drug discovery?

Answer 1

Discovery Phases: Target identification → screening → hit-to-lead → lead optimisation → preclinical development.

Question 2

What is lead optimisation?

Answer 2

Lead Optimisation: Refines potency, selectivity, pharmacokinetics, and safety

Question 3

what are the ideal orally available drug requirements

Answer 3

High bioavailability, metabolic stability, and minimal toxicity.

Question 4

Describe the pharmocokinetic plasma profile

Answer 4

Generated by analysing drug concentration over time.
Used to evaluate absorption, distribution, metabolism, and elimination (ADME).

Question 5

What is the drug like property assessment?

Answer 5

Predictive: Lipinski’s Rule of 5, in silico modelling.
Experimental: Solubility, permeability, and metabolic stability assays.