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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The retrospective identification of the drug targets that underlie an observed phenotypic response is termed Target Deconvolution. Target Deconvolution can be achieved by numerous methods including; Affinity Chromatography, Expression-Cloning, Protein Microarray, ‘reverse transfected’ Cell Microarray, and Biochemical Suppression

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Early Drug Discovery and Development Guidelines: For Academic Researchers, Collaborators, and Start- up Companies

Published by EATRIS

Target Validation Drug DevelopmentNCATSNIHResearch and Drug DevelopmentDrug Discovery GuidelineSmall MoleculeDrug Repurposing

This manual contains guidelines to develop therapeutic hypotheses, target and pathway validation, proof of concept criteria and generalized cost analyses at various stages of early drug discovery. Various decision points in developing a New Chemical Entity (NCE), description of the exploratory Investigational New Drug (IND) and orphan drug designation, Drug Repurposing and drug delivery technologies are also described and geared toward those who intend to develop new drug discovery and development programs.

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Assay Development and Screening Technology (ADST)

Published by NCATS

NCATSHigh Throughput ScreeningSmall Molecule

One of the first steps in the drug development process is creating test systems — called assays — on which researchers assess the effects of chemical compounds on cellular, molecular or biochemical processes of interest. At NCATS, the experts in the Assay Development and Screening Technology (ADST) program work to optimize assays requested or submitted by the biomedical research community for high-throughput small-molecule screening

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