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Drug Kinetics – Multimedia

Effects of Gender, age and Ethnicity on Human Cytochrome P450 Activity content piece image
Poster

Effects of Gender, age and Ethnicity on Human Cytochrome P450 Activity

The expression of CYP enzymes is influenced by both endogenous and exogenous factors. The aim of this analysis was to evaluate whether the age, gender, or ethnicity of the donor should influence the selection of human liver microsomes for drug metabolism studies, as well as whether cigarette smoking and alcohol consumption are reliable indicators of elevated CYP1A2 and CYP2E1 activity, respectively.
A Software-Aided Approach to Reducing the Synthetic Burdens of Lead Structure Optimization content piece image
Poster

A Software-Aided Approach to Reducing the Synthetic Burdens of Lead Structure Optimization

Following the identification of a lead compound, the usual next step is optimization of that lead via slight structural modifications to improve or retain potency while simultaneously minimizing liabilities. Achieving this balance of required properties is a significant challenge. ACD/Structure Design Suite is a software tool that significantly helps the medicinal compounds that are expected to produce analogs with improved selected physicochemical properties.
Combination of in Vitro Caco-2 and Aqueous Solubility Screens with in Silico Physiological Modelling for the Prediction of Human Intestinal Absorption in Early Drug Discovery content piece image
Poster

Combination of in Vitro Caco-2 and Aqueous Solubility Screens with in Silico Physiological Modelling for the Prediction of Human Intestinal Absorption in Early Drug Discovery

With the increasing application of high-throughput assays for the determination of the in vitro ADME properties of compounds in lead identification and optimization, there is a growing need for efficient and cost-effective methods for interpreting theresulting data to enable well-informed selection to be made for compound progression.
Rapid Solution Exchange and Ligand-Gated Channel Studies on the PatchXpress 7000A Automated Patch Clamp System content piece image
Poster

Rapid Solution Exchange and Ligand-Gated Channel Studies on the PatchXpress 7000A Automated Patch Clamp System

The PatchXpress® 7000A patch clamp system is an automated electrophysiology workstation that allows users to increase throughput of research quality recordings and to measure ion channel activity from nearly any channel type.
Reducing the Synthetic Burdens of Lead Structure Optimization: A Novel Software-Aided Approach content piece image
Poster

Reducing the Synthetic Burdens of Lead Structure Optimization: A Novel Software-Aided Approach

At the later stages of drug optimization it is beneficial to augment the select ADME properties of leads by making small structural changes that do not introduce any negative effects on the activity or toxicity profiles. By combining physicochemical property predictors and a critically evaluated database of biologically-acceptable substituents, the synthetic chemist can evaluate and reduce the number of derivative compounds that need to be synthesized to achieve optimal drug-like properties.
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