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Flashcards in Intro to drug discovery Deck (12):
1

What is the difference between drug discovery and drug development?

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

2

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

True

3

What is meant be a 'hit'?

A compound with biological activity in a basic model

4

What is meant by a 'lead'?

A compound with biological activity in in-vitro models

5

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

False - more potent and permeates membranes

6

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

solubility decreases
protein-binding, metabolism and toxicity increase -

7

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

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

8

a log d < 0 indicates what?

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

9

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

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

10

logD is dependent on pH. True or false?

True

11

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

True

12

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

False - equal to or less than logP