Intro to drug discovery

Question 1

What is the difference between drug discovery and drug development?

Answer 1

Drug discovery is finding a compound that has a suitable profile for advancing to clinical trials.
Drug development is testing this agent to demonstrate that it is suitable for use in the clinic

Question 2

less than 10% of compounds that enter clinical trials are likely to be approved for clinical use. True or false?

Answer 2

True

Question 3

What is meant be a ‘hit’?

Answer 3

A compound with biological activity in a basic model

Question 4

What is meant by a ‘lead’?

Answer 4

A compound with biological activity in in-vitro models

Question 5

As lipophilicity of a drug increases, it’s less likely to be potent and therefore doesn’t permeate membranes. True or false?

Answer 5

False - more potent and permeates membranes

Question 6

As lipophilicity increases, what happens to the solubility, metabolism and protein binding and toxicity of the drug?

Answer 6

solubility decreases

protein-binding, metabolism and toxicity increase -

Question 7

a log d > 0 indicates that the drug is hydrophilic. True or false?

Answer 7

False - indicates that more compound is in organic state than aq and therefore drug is hydrophobic

Question 8

a log d < 0 indicates what?

Answer 8

more compound is in aq than organic phase and so the drug is hydrophilic

Question 9

Increasing ionisation of a compound will increase log d. True or false?

Answer 9

False - increasing ionisation will pull more of the drug into aq phase, decreasing log d

Question 10

logD is dependent on pH. True or false?

Answer 10

True

Question 11

For neutral compounds, logD = logP. True or false?

Answer 11

True

Question 12

For ionisable compounds, logD equal to or greater than logP. True or false?

Answer 12

False - equal to or less than logP