Drug discovery and development: Role of basic biological research

Published by Alzheimers Dement (N Y).

Drug DiscoveryTarget Validation

This article provides a brief overview of the processes of drug discovery and development. The aim is to help scientists whose research may be relevant to drug discovery and/or development to frame their research report in a way that appropriately places their findings within the drug discovery and development process and thereby support effective translation of preclinical research to humans.

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Estimating human ADME properties, pharmacokinetic parameters and likely clinical dose in drug discovery

Published by Expert Opinion on Drug Discovery

PK or PDDose EstimationADMELead OptimisationTarget ValidationPharmacokinetics

The aim of this article is to provide a framework to facilitate apposite human PK and dose predictions as a continuum during drug discovery. Firstly, for early Dose Estimation to guide compound design, accelerate decision-making and focus strategy, a simple PK model is proposed based on achieving and maintaining average steady-state concentrations (Css,av) related to a measure of efficacious concentration. A toolbox of methods for the prediction of PK parameters is provided with consideration of the appropriate and effective use. Finally, advances in the understanding of compound properties and TPP will inform model selection for dose projection.

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Exploring The Structure-Activity Relationship (SAR) of Drugs


Lead OptimisationTarget ValidationIn Silico ToolStructure-Activity Relationship

The Structure-Activity Relationship (SAR) aids in understanding various aspects of drug discovery, from screening drug candidates to optimizing their properties. The effective biological activity is contributed by the various geometric and electrostatic interactions. This article introduce in a briefly way the diferent uses of The Structure-Activity Relationship (SAR) in drug discovery.

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