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Drug Discovery: Overview

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...

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Updated: Dec 25, 2025

An Organotypic High Throughput System for Characterization of Drug Sensitivity of Primary Multiple Myeloma Cells

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Published on: July 15, 2015

Multiparametric Assays for Accelerating Early Drug Discovery.

Alexander Herholt¹, Sabrina Galinski¹, Philipp E Geyer²

¹Department of Psychiatry and Psychotherapy, University Hospital, LMU Munich, Nussbaumstr. 7, 80336 Munich, Germany; Systasy Bioscience GmbH, Balanstr. 6, 81669, Munich, Germany.

Trends in Pharmacological Sciences

|April 1, 2020

Summary

Drug discovery faces high failure rates due to efficacy and safety issues, especially in complex diseases. Innovative assays and mass spectrometry proteomics can improve profiling of drug candidates for better drug discovery and personalized medicine.

Keywords:

CRISPR/Cas9 barcoding complex diseases compound profiling patient-derived disease model phenotypic screening

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Last Updated: Dec 25, 2025

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Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications

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Published on: January 27, 2014

Area of Science:

Biochemistry
Pharmacology
Biotechnology

Background:

Drug discovery campaigns suffer from high attrition rates, primarily due to efficacy and safety concerns of candidate drugs.
Genetically complex diseases exacerbate attrition due to limited understanding of drug actions on targets and pathways.
Elucidating complex cellular signaling networks requires innovative technologies for better drug profiling.

Purpose of the Study:

To discuss advancements in genetically encoded multiparametric assays and mass spectrometry (MS)-based proteomics.
To highlight the potential of these technologies in profiling multifactorial drug actions.
To promote improved drug discovery and personalized medicine.

Main Methods:

Genetically encoded multiparametric assays for profiling compound actions.
Mass spectrometry (MS)-based proteomics for target and pathway analysis.
Utilizing disease-relevant cellular systems to assess drug candidates.

Main Results:

Genetically encoded assays offer multiparametric profiling of drug candidates.
MS-based proteomics provides comprehensive analysis of target engagement and pathway modulation.
These toolkits enhance the understanding of drug actions in complex biological systems.

Conclusions:

Innovative technologies like genetically encoded assays and MS-based proteomics are crucial for overcoming drug discovery attrition.
These methods enable better profiling of drug candidates' effects on targets and pathways.
Advancements facilitate more effective drug discovery and the development of personalized medicine approaches.