iClicker Questions

Which of the following statements best describes the relationship between SAR and SPR during small molecular drug development?

SAR is focused on optimizing compound potency and SPR is focused on optimizing the drug-like properties of the compound

What information does the Hammett Substituent Constant for a given functional group give you?

the electron withdrawing properties of the FG when it is a substituent on an aromatic ring

Which of the follow statements best describes the point of determining structure-activity relationships during the drug discovery process?

to learn what structural features of the compound are important so that we can modify these regions of the scaffold to make more potent analogues

During the drug development process, when should a medicinal chemist optimize SPR for their scaffold?

side by side with optimizing potency

Which of the following statements best describes the importance of balancing the hydrophobicity/hydrophilicity of a potential small molecule drug?

an optimal small molecule drug is hydrophobic enough to bind a protein binding site and hydrophilic enough to be water soluble and orally bioavailable

Which of the following best describes a prodrug?

an inactive precursor that relies on natural mechanisms to be converted to the active drug form

Which of the following types of prodrugs is converted to the active form of the drug in the target therapeutic tissue?

type IA

Which of the following statements best describes the process of Phase 1 and Phase 2 drug metabolism?

Phase 1 primarily installs a small hydrophilic FG that can then be conjugated w/ a larger hydrophilic group during Phase 2 to enhance water solubility and increase excretion

Which of the following best describes the role OCTs play in drug transport and metabolism?

OCTs are Phase 0 uptake transporters that have small organic cations as their primary substrates

The enzymes responsible for metabolizing quinones via reduction are:

NQOs

Which of the following is grouped correctly for Phase 2 rxns, enzymes, and cofactors?

Glucuronidation, UGTs, UDP-GA

What is the most likely reason fluorine is incorporated into a compound?

to enhance stability of the drug by decreasing the CYP450 metabolism

Which of the following statements about protein-protein interactions (PPIs) as emerging targets is FALSE?

PPIs are excellent drug targets because there are multiple binding spots at the PPI interface where drugs can bind

Which of the following best describes why PROTACs have emerged as a promising new class of small molecule therapeutics?

PROTACs are easier to synthesize than small molecules and are generally easier to prepare at the manufacturing level

Why do covalent inhibitors generally exhibit higher potency against their target when compared to reversible inhibitors?

there is no on/off rate for a covalent inhibitor → as soon as inhibitor binds, it inactivates the target