18 Questions
What is the main focus of methods for assessing druggability mentioned in the text?
Assessing the likelihood of proteins binding drug-like molecules
Which algorithm is specifically mentioned as being trained on a set of binding sites from the Protein Data Bank?
PocketFinder
What does the text suggest as an issue with ligand/structure-based druggability assessment methods?
They are not applicable when crystal structures are unavailable
Which database is NOT mentioned as a source for high affinity drug-like compounds in the text?
TTD
What is a key property used in structure-based prediction methods to assess druggability?
Surface area
Why are methods needed to prioritize proteins in the human genome according to the text?
To assess proteins that may be 'druggable' without crystal structures
What are the key properties a protein's binding site should have to bind drug-like compounds?
Appropriate size, buried, not too polar, large exposed polar sites
Why is it important to assess druggability when identifying potential drug targets?
To avoid failure in later stages due to poor pharmacokinetic properties of compounds
How can protein druggability be assessed based on structural analysis?
By checking the protein Data Bank for predictions
What is one reason choosing a target that doesn't bind small molecules can lead to failure?
Potential failure in identifying clinical candidates
What percentage of human genome is estimated to be druggable with a small molecule approach?
~15%
In assessing druggability, what type of studies are used to relate genes/proteins to disease?
A combination of sequencing/GWAS studies, expression studies, and proteomics/metabolomics studies
What is another term sometimes used instead of 'druggability'?
Ligandability
Which of the following is NOT one of Lipinski's Rule of Five for drug-likeness?
LogP < 3
What do the Lipinski's Rule of Five suggest may lead to poor absorption and permeability?
High number of H-bond Acceptors
Which term describes the likelihood of finding orally bioavailable small molecules that bind to a particular target in a disease-modifying way?
Druggability
What is important in assessing ligand-based druggability?
Hydrophobicity
Which parameter is crucial in determining the ability of a protein target to bind small molecules with high affinity?
H-bond interactions between the ligand and protein
Learn about what druggability is and its importance in drug discovery. Explore different methods such as precedence-based, structure-based, and future-based approaches. Discover the concept of the druggable genome and its applications in target prioritization.
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