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Related Concept Videos

Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Principles of Drug Action01:24

Principles of Drug Action

Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Drug-Receptor Bonds01:25

Drug-Receptor Bonds

Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
In...

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Related Experiment Video

Updated: May 26, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
05:28

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction

Published on: August 27, 2019

What makes a good drug target?

Isabella Gashaw1, Peter Ellinghaus, Anette Sommer

  • 1Global Drug Discovery - Target Discovery, Bayer HealthCare, Muellerstrasse 178, 13342 Berlin, Germany. isabella.gashaw@bayer.com

Drug Discovery Today
|December 14, 2011
PubMed
Summary

Identifying effective drug targets is crucial for developing novel therapeutics, especially for unmet medical needs. This article outlines key properties of a good drug target from a pharmaceutical company

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Last Updated: May 26, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
05:28

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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Area of Science:

  • Drug discovery and development
  • Pharmaceutical sciences
  • Molecular pharmacology

Background:

  • Novel therapeutics are essential for addressing areas with high unmet medical needs.
  • While biologicals have expanded druggable molecules, suitable drug targets remain limited.
  • Current target assessment involves experimental, mechanistic, and pharmacological studies.

Purpose of the Study:

  • To define the key properties of an ideal drug target.
  • To provide a pharmaceutical company's perspective on drug target selection.
  • To emphasize the importance of early theoretical molecular druggability assessment.

Main Methods:

  • Review of current practices in drug target identification and assessment.
  • Analysis of factors influencing drug target selection in pharmaceutical companies.
  • Discussion of theoretical molecular druggability assessment and its role.

Main Results:

  • Drug target assessment requires more than just experimental validation.
  • Early evaluation of potential side effects and commercialization opportunities is critical.
  • A comprehensive approach is needed to identify and assess drug targets effectively.

Conclusions:

  • Defining a good drug target involves a multifaceted evaluation.
  • Pharmaceutical companies prioritize targets with a strong theoretical and commercial outlook.
  • Integrating early-stage assessments can improve the success rate of novel therapeutics.