Drug Discovery: Finding a Lead Ch 12

Question 1

Hit

Answer 1

compound that is active in an assay

Question 2

Lead

Answer 2

optimizable compound that is active on an assay.

Question 3

4 Drug targets

Answer 3

Lipids, Proteins, Nucleic acids, Carbohydrates

Question 4

Target selectivity between species

Answer 4

Antibacterial and antiviral agents

Identify targets that are unique or identify shared targets that are significantly different

Question 5

Target selectivity within body

Answer 5

Different enzyme, receptors, etc.
Different receptor types and subtypes, isozymes.
Different organs.

Question 6

In vivo tests

What does it measure?

Answer 6

Carried out on live animals or humans to measure drug ability to interact with target and its ability to reach target and identify side effects.

Question 7

Potency

Answer 7

concentration required to produce 50% of the maximum possible effect

Question 8

Therapeutic ratio

Answer 8

compares the dose level of drug required to produce desired effect in 50% of test sample vs. dose level that is lethal in 50% of sample

Question 9

In vitro tests

What does it measure?

Answer 9

Not carried out in animals/humans.

Measures interaction drug with target only. Cannot identify prodrugs

Question 10

Enzyme inhibition test

Answer 10

Identify competitive or noncompetive inhibition. Measures IC50 (concentration of inhibitor required to reduce enzyme activity by 50%)

Question 11

Testing with receptors (3 measurements)

Answer 11

Affinity: strength with which compound binds to receptor.
Efficacy: measure of maximum biochemical effect resulting from binding.
Potency-concentration required to produce 50% of the maximum possible effect.