Drug Discovery Process

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What is the primary goal of High-Throughput Screening (HTS)?

To validate a target for drug discovery

To optimize a lead compound for clinical trials

To identify a compound with desired activity (correct)

To develop an assay for a specific target

What is the term used to describe a compound with desired activity in a compound screen?

Modulator

Target

Lead compound

Hit (correct)

What is the purpose of assay development in the drug discovery process?

To develop a method to test compounds against a specific target (correct)

To conduct clinical trials

To validate a target for drug discovery

To identify a lead compound

What is the typical format used for conducting assays in High-Throughput Screening?

96-well plates Signup and view all the answers

What is the next step in the drug discovery process after target validation?

Assay development Signup and view all the answers

What is the acronym for the regulatory body responsible for approving new drugs in the United States?

FDA Signup and view all the answers

What is the purpose of a focused-based screen in drug discovery?

To initiate a project based on a compound with published activity against the target Signup and view all the answers

What is the main advantage of homogeneous assays?

They are simpler and less expensive Signup and view all the answers

What is the main difference between heterogeneous and homogeneous assays?

Number of steps involved Signup and view all the answers

What is the limitation of biochemical assays?

Not all targets can be purified or prepared Signup and view all the answers

What is the purpose of enzymatic assays?

To measure enzymatic activity and inhibition Signup and view all the answers

What is the purpose of receptor binding assays?

To measure the binding of ligand molecules to receptors Signup and view all the answers

What is the definition of EC50 in saturation binding?

The concentration of compound required for 50% receptor occupancy Signup and view all the answers

What is the purpose of competition binding in biochemical assays?

To determine the presence of selectivity for a particular ligand Signup and view all the answers

What is the purpose of using radioligands in receptor binding assays?

To measure the binding of ligand molecules to receptors Signup and view all the answers

What is the first step in signal transduction by a GPCR?

Signal transduction by a GPCR begins with an inactive G protein Signup and view all the answers

What is the result of the G protein subunits detaching from the receptor?

Initiation of signaling pathways Signup and view all the answers

What is the purpose of using [35S]GTPγS in the binding assay?

To measure the level of radiolabeled GTPγS bound to the Gα subunit Signup and view all the answers

What is the consequence of the radiolabeled GTPγS binding to the Gα subunit?

The reaction is terminated, and the radioactivity increases Signup and view all the answers

What does the level of radiolabeled GTPγS bound to the Gα subunit indicate?

The efficacy of the compound Signup and view all the answers

What is the consequence of agonist stimulation on guanine nucleotide exchange at G-proteins?

An increase in guanine nucleotide exchange Signup and view all the answers

What type of enzyme immunoassay is ELISA?

Solid-phase Signup and view all the answers

What is the purpose of adding a substance containing the enzyme's substrate in an ELISA?

To produce a detectable signal Signup and view all the answers

What is the purpose of protein denaturation in Western blots?

To separate proteins by size Signup and view all the answers

What is the function of the primary antibody in Western blots?

To recognize and bind to a specific target protein Signup and view all the answers

What is the purpose of using a spectrometer in ELISA?

To give quantitative values for color strength Signup and view all the answers

What is the type of assay that uses antibodies directed against a protein to detect its presence in a sample?

Cell-based ELISA Signup and view all the answers

What is the purpose of the 125I-Tyr1 som-14 in the receptor binding experiment?

To label the peptide and measure the receptor binding Signup and view all the answers

What is the role of Gα in the signal transduction pathway?

To dissociate from the Gβ and Gγ subunits Signup and view all the answers

What is the purpose of the G protein assay in the biochemical assays?

To measure the signal transduction by a GPCR Signup and view all the answers

What is the outcome of the competition binding analysis?

Displacement of 125I-som-14 (%) by the test compounds Signup and view all the answers

How were the CHO cells prepared for the receptor binding experiment?

By washing them with buffer Signup and view all the answers

What was the outcome of the screening process?

Two compounds were found to be promising for drug development Signup and view all the answers