Podcast
Questions and Answers
What is the purpose of high throughput screening (HTS) in drug development?
What is the purpose of high throughput screening (HTS) in drug development?
To test a vast number of compounds for biological activity
Describe the process of identifying the active compound in an equilibrium reaction.
Describe the process of identifying the active compound in an equilibrium reaction.
Freezing the equilibrium reactions and performing an irreversible reaction to convert all equilibrium products to stable compounds
How are HTS assays mainly conducted?
How are HTS assays mainly conducted?
Mostly optical assays (fluorescence, luminescence, absorbance)
What is the benefit of using multi-well plates with a higher number of wells in HTS assays?
What is the benefit of using multi-well plates with a higher number of wells in HTS assays?
Explain the role of carbonic anhydrase in the DCS reaction mentioned in the text.
Explain the role of carbonic anhydrase in the DCS reaction mentioned in the text.
What is the significance of using irreversible reactions in shifting the equilibrium towards the active compound?
What is the significance of using irreversible reactions in shifting the equilibrium towards the active compound?
What is the purpose of using photolithography in combinatorial chemistry?
What is the purpose of using photolithography in combinatorial chemistry?
Explain the concept of Safety Catch and acid-labile linker in solid phase extraction.
Explain the concept of Safety Catch and acid-labile linker in solid phase extraction.
How does Dynamic Combinatorial Chemistry (DCS) differ from typical mix and split synthesis?
How does Dynamic Combinatorial Chemistry (DCS) differ from typical mix and split synthesis?
What role does the photolabile protecting group play in peptide synthesis using photolithography?
What role does the photolabile protecting group play in peptide synthesis using photolithography?
How are peptide microsequencing and bead-based synthesis related in combinatorial chemistry?
How are peptide microsequencing and bead-based synthesis related in combinatorial chemistry?
Explain the concept of peptide chains with different sequences in parallel synthesis using masks.
Explain the concept of peptide chains with different sequences in parallel synthesis using masks.
What are the two ways of generating an array of compounds for finding hits and leads in drug discovery?
What are the two ways of generating an array of compounds for finding hits and leads in drug discovery?
What is the advantage of Parallel Synthesis (PS) over Combinatorial Synthesis (CS) in terms of structure identification?
What is the advantage of Parallel Synthesis (PS) over Combinatorial Synthesis (CS) in terms of structure identification?
Why is Combinatorial Synthesis (CS) valuable for finding leads in drug discovery?
Why is Combinatorial Synthesis (CS) valuable for finding leads in drug discovery?
What was the first example of solid-phase synthesis mentioned in the text?
What was the first example of solid-phase synthesis mentioned in the text?
Why is the Merrifield resin rarely used these days in peptide synthesis?
Why is the Merrifield resin rarely used these days in peptide synthesis?
What are the names of more modern resins used in peptide synthesis?
What are the names of more modern resins used in peptide synthesis?
What type of molecules were early solid-phase synthesis efforts concentrated on, despite their poor pharmacokinetic properties?
What type of molecules were early solid-phase synthesis efforts concentrated on, despite their poor pharmacokinetic properties?
What is the role of benzodiazepines like Valium as positive allosteric effectors?
What is the role of benzodiazepines like Valium as positive allosteric effectors?
How are spider-like scaffolds used in the design of compound libraries?
How are spider-like scaffolds used in the design of compound libraries?
What is the importance of having evenly spaced arms in spider-like scaffolds for compound library design?
What is the importance of having evenly spaced arms in spider-like scaffolds for compound library design?
What are the other multi-component reaction reaction type that have been used to generate large compound libraries?
What are the other multi-component reaction reaction type that have been used to generate large compound libraries?
How does fluorous solid-phase extraction (F-SPE) differ from basic column extraction?
How does fluorous solid-phase extraction (F-SPE) differ from basic column extraction?
What is the purpose of using scavenger resins in Parallel Synthesis (PS) work up?
What is the purpose of using scavenger resins in Parallel Synthesis (PS) work up?
Describe the Catch-and-Release strategy mentioned in the text.
Describe the Catch-and-Release strategy mentioned in the text.
In amide synthesis using carbodiimide urea, what are the three main components involved?
In amide synthesis using carbodiimide urea, what are the three main components involved?
How can excess amine be efficiently removed after forming the urea derivative in a reaction?
How can excess amine be efficiently removed after forming the urea derivative in a reaction?
What are the advantages of using microfluidics in parallel synthesis?
What are the advantages of using microfluidics in parallel synthesis?
Explain the mix-and-split method in combinatorial synthesis.
Explain the mix-and-split method in combinatorial synthesis.
What is the purpose of combinatorial synthesis (CS) in drug discovery?
What is the purpose of combinatorial synthesis (CS) in drug discovery?
How does microwave-assisted organic synthesis (MAOS) differ from conventional synthesis?
How does microwave-assisted organic synthesis (MAOS) differ from conventional synthesis?
What is the role of the mix-and-split method in generating compounds in combinatorial synthesis?
What is the role of the mix-and-split method in generating compounds in combinatorial synthesis?
How does the mix-and-split method benefit the synthesis of a dipeptide from 5 amino acids?
How does the mix-and-split method benefit the synthesis of a dipeptide from 5 amino acids?
What is the purpose of using bifunctional linkers like SCAL in compound synthesis?
What is the purpose of using bifunctional linkers like SCAL in compound synthesis?
Explain the concept of compound tagging in the context of a 3-step synthesis using SCAL.
Explain the concept of compound tagging in the context of a 3-step synthesis using SCAL.
How can the target molecule on the Trp residue be released after the last synthetic step?
How can the target molecule on the Trp residue be released after the last synthetic step?
What is the significance of performing syntheses with beads that harbor bifunctional linkers in compound identification?
What is the significance of performing syntheses with beads that harbor bifunctional linkers in compound identification?
In a 3-step synthesis using SCAL, what does each tag represent?
In a 3-step synthesis using SCAL, what does each tag represent?
How does the use of bifunctional linkers like SCAL contribute to compound synthesis and identification?
How does the use of bifunctional linkers like SCAL contribute to compound synthesis and identification?
What is the purpose of peptide microsequencing in combinatorial chemistry?
What is the purpose of peptide microsequencing in combinatorial chemistry?
How does photolithography contribute to peptide synthesis?
How does photolithography contribute to peptide synthesis?
What are the key aspects of Dynamic Combinatorial Chemistry (DCS)?
What are the key aspects of Dynamic Combinatorial Chemistry (DCS)?
Explain the concept of Safety Catch in solid-phase extraction.
Explain the concept of Safety Catch in solid-phase extraction.
How does the process of photolithography allow for the creation of peptide chains with different sequences?
How does the process of photolithography allow for the creation of peptide chains with different sequences?
What is the main advantage of Parallel Synthesis (PS) over Combinatorial Synthesis (CS) in terms of structure identification?
What is the main advantage of Parallel Synthesis (PS) over Combinatorial Synthesis (CS) in terms of structure identification?
What is the purpose of High Throughput Screening (HTS) in drug development?
What is the purpose of High Throughput Screening (HTS) in drug development?
How are HTS assays mainly conducted?
How are HTS assays mainly conducted?
Why was the sulfonamide compound significantly amplified in the DCS reaction?
Why was the sulfonamide compound significantly amplified in the DCS reaction?
Describe the process of identifying the active compound in an equilibrium reaction.
Describe the process of identifying the active compound in an equilibrium reaction.
What is the significance of using irreversible reactions in shifting the equilibrium towards the active compound?
What is the significance of using irreversible reactions in shifting the equilibrium towards the active compound?
What are the main features of High Throughput Screening (HTS) systems like the UltraHTS system at Bristol-Myers Squibb?
What are the main features of High Throughput Screening (HTS) systems like the UltraHTS system at Bristol-Myers Squibb?
