Flashcards in Intro to drug discovery Deck (12):
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
less than 10% of compounds that enter clinical trials are likely to be approved for clinical use. True or false?
What is meant be a 'hit'?
A compound with biological activity in a basic model
What is meant by a 'lead'?
A compound with biological activity in in-vitro models
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
As lipophilicity increases, what happens to the solubility, metabolism and protein binding and toxicity of the drug?
protein-binding, metabolism and toxicity increase -
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
a log d < 0 indicates what?
more compound is in aq than organic phase and so the drug is hydrophilic
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
logD is dependent on pH. True or false?
For neutral compounds, logD = logP. True or false?