MDC Connects: A Guide to Drug Discovery

Published by Medicines Discovery Catapult

Drug DiscoveryTarget IdentificationSmall Molecules

This guideline is a summary presentation from the Medicines Discovery Catapult (MDC) webinars. The aim was to create a resource of modern drug discovery knowledge to support small companies who are developing their own medicines. The guideline is focused on preclinical research with an emphasis on small molecules in the following topics:
• What makes, and how to identify, a good target
• Methods to identify the chemical compound which would become the drug
• How to optimise that drug
• How to test it works in models of disease
• And how to demonstrate that it would be safe to dose in humans

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

Published by EATRIS

Research and Drug DevelopmentDrug Discovery GuidelineSmall MoleculeDrug RepurposingTarget Validation Drug DevelopmentNCATSNIH

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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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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Genetic-Driven Druggable Target Identification and Validation

Published by Trends Genet.

Target IdentificationGWAS AssociationGenetic ToolboxExpression Quantitative Trait Locus

This article reviews the opportunities and challenges, and infer criteria for the optimal use of genetic findings in the drug discovery pipeline. Choosing the right biological target is the critical primary decision for the development of new drugs. Systematic genetic association testing of both human diseases and quantitative traits, along with resultant findings of coincident associations between them, is becoming a powerful approach to infer drug targetable candidates and generate in vitro tests to identify compounds that can modulate them therapeutically

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Functional Genomics Lab

Published by NCATS

NCATSTarget IdentificationRNAi Screening

NCATS’ Functional Genomics Lab is designed to develop and improve RNAi Screening approaches to better understand gene function and identify treatment targets. Gene silencing through RNAi has emerged as a powerful tool for understanding gene function. Over the past several years, high-throughput RNAi screens have illuminated a wide variety of biological processes, ranging from genes that affect the activity of therapeutic agents to novel components of signaling pathways.

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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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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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