a) Explain the significance of hERG binding. b) Which of the compounds 1-8 is li
ID: 3518959 • Letter: A
Question
a) Explain the significance of hERG binding.
b) Which of the compounds 1-8 is likely to have the worst bioavailability? Explain your answer.
c) Which of the compounds 1-8 is likely to have the greatest toxicity? Explain your answer.
d) Which would you choose for further development?
6) In the following table, the results from a series of assays on compounds 1-8 are shown. gp160 assay is an anti HIV assay which determines the concentration of to inhibit HIV replication. (10 marks) The compound required hERG binding iC50 (uM)b 0.01 gpl 60, IC50 (nM)"Explanation / Answer
a) hERG binding helps in knowing the potent antagonist drugs to use in treatment of HIV.the use of a pharmacophore model of the hERG channel and a high throughput binding assay for the hERG channel are described that were critical to elucidate SAR to overcome hERG liabilities.
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