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

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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Open access In Silico Tools to predict the ADMET profiling of drug candidates

Published by Expert Opinion on Drug Discovery

Drug DiscoveryTarget IdentificationLead OptimisationIn Silico Tool

This review meticulously encompasses the fundamental functions of open access in silico prediction tools (webservers and standalone software) and advocates their use in drug discovery research for the Safety and reliability of any candidate-drug. This review also aims to help support new researchers in the field of drug design.

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

Published by Expert Opinion on Drug Discovery

ADMELead OptimisationTarget ValidationPharmacokineticsPK or PDDose Estimation

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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