BPS 2110 Lecture Notes - Lecture 5: High-Performance Liquid Chromatography, Adme, Partition Coefficient

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Potency measure of [drug] required to achieve an effect. Drug potency in binding is an eqm between drug dissolved in water and drug dissolved in protein. Use information to design the next compound to test. Bioavailable: % drug enters blood stream after oral dose. Drugs in solution are surrounded by water that are stripped away as the drug enters the binding sirte. Requires energy because polar drugs cling to water. Binding pockets and drugs are often very lipophilic facilitates water removal and ligand binding facilitates de-solvation and improves binding to target. Easier to isolate if both pocket and drug are lipophilic. Not all drug molecules will pass each barrier to target but try to maximize the amount that does. Properties of the drug control how easily it passes these barriers (adme) Drug must be water soluble, able to survive strong acid but have little or no drug absorbed.

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