Answered step by step
Verified Expert Solution
Question
1 Approved Answer
Consider issues related to a high throughput screen in 384-well plates to find inhibitors of the enzyme Factor XIa. Consider issues related to a high
Consider issues related to a high throughput screen in 384-well plates to find inhibitors of the enzyme Factor XIa.
Consider issues related to a high throughput screen in 384-well plates to find inhibitors of the enzyme Factor XIa. A) Identify a suitable fluorogenic peptide for this assay. B) Assuming Km=47uM and kcat=0.72s1 under the buffer conditions of the assay, calculate the time needed for 50% conversion of substrate if reactions are run at: [S(t=0)]=2uM[E(t=0)]=6nM C) Calculate the time needed for 50% conversion of substrate if a competitive inhibitor (KI=1.3uM) is used at a concentration of 7uM. D) Plot the F.I.(t) for the reaction in the absence and presence of 7 uM inhibitor. Assume the F.I. of the product is 15,000 F.I./uM in the assay reader. Assume the substrate has a background fluorescence intensity 800 F.I. at 2 uM. E) Find a structure of a Factor Xia inhibitor and give its IC50 or Ki. Comment on the compound's Lipinski ParametersStep by Step Solution
There are 3 Steps involved in it
Step: 1
Get Instant Access to Expert-Tailored Solutions
See step-by-step solutions with expert insights and AI powered tools for academic success
Step: 2
Step: 3
Ace Your Homework with AI
Get the answers you need in no time with our AI-driven, step-by-step assistance
Get Started