Exam 4 Flashcards
What is drug affinity?
How well the drug binds to the receptor
What is drug efficacy?
How well the drug produces the desired effect
What is drug potency?
Compares the relative affinity of a drug to a receptor compared to other drugs
Drug must out compete the native ligand to induce an effect
Where do most drugs fail during development?
- Most drugs fail during the discovery phase
- ~90% of all drugs fail in clinical testing (1:10,000 success rate)
What is the Lipinski Rule of 5?
- Tool used to measure a new chemical entity (NCE) bioavailability
Rules:
1. < 10 hydrogen bond donors (NH, OH) or acceptors (N, O)
2. < 500 Da molecular weight
3. < 5 Calculated partition coefficient (cLogP)
4. Not more than 1 toxicophore
Violation of more than one rule predicts the NCE non-orally available
What do hydrogen bonds bind to on a receptor?
Polar, acidic, and basic groups
Determine the various intermolecular forces for Dibucaine?
What are the structural alert drugs and there strucure?
Napthelene is the only polycyclic aromatic that is ok
Thiophenes are bad due to sulfur oxidation
NAP AT night
What is the measure of a dalton?
What is considered a “small” drug?
- Da = g/mol
- 500 da or less
Define an acid and base (Bronsted-Lowry)?
- Acid - proton donor
- Base - proton acceptor
Determine the acid, base, conjugate acid, and conjugate base of the following reaction?
Determine the acid, base, conjugate acid, and conjugate base of the following reaction?
Define amphoteric and what compound has this property?
Amphoteric means a compound can act as an acid or a base like water
What defines a strong acid? weak acid?
What are the strong acids?
Stong acids completely ionize in water
Weak acids partially ionize in water
Bring Clean ClOthes If NOt Swimming
What defines a strong base? weak base?
What are the strong bases?
Strong bases completely ionize in water
Weak bases partially ionize in water
LiNK BaCS