Abstract
This review aims to give an overview of current good practice in the prosecution of Lead Generation. It will assess experiences across the field as judged from the contents of the limited number of peer-review disclosures to date. It will also rely heavily on the experiences of the authors from many campaigns within this organisation. Its focus will be on the assembly of an appropriate compound collection for application in High Throughput Screening (HTS), the prosecution of HTS, the profiling of HTS output and, lastly the Hit-to-Lead optimisation of selected HTS output. Excluded from the scope are detailed aspects of library design [1], parallel synthesis [2], virtual library applications [3], virtual screening [4] and fragment screening [5] approaches, all of which have been the subject of recent reviews.
Current Topics in Medicinal Chemistry
Title: Components of Successful Lead Generation
Volume: 5 Issue: 4
Author(s): Andrew M. Davis, David J. Keeling, John Steele, Nicholas P. Tomkinson and Alan C. Tinker
Affiliation:
Abstract: This review aims to give an overview of current good practice in the prosecution of Lead Generation. It will assess experiences across the field as judged from the contents of the limited number of peer-review disclosures to date. It will also rely heavily on the experiences of the authors from many campaigns within this organisation. Its focus will be on the assembly of an appropriate compound collection for application in High Throughput Screening (HTS), the prosecution of HTS, the profiling of HTS output and, lastly the Hit-to-Lead optimisation of selected HTS output. Excluded from the scope are detailed aspects of library design [1], parallel synthesis [2], virtual library applications [3], virtual screening [4] and fragment screening [5] approaches, all of which have been the subject of recent reviews.
Export Options
About this article
Cite this article as:
Davis M. Andrew, Keeling J. David, Steele John, Tomkinson P. Nicholas and Tinker C. Alan, Components of Successful Lead Generation, Current Topics in Medicinal Chemistry 2005; 5 (4) . https://dx.doi.org/10.2174/1568026053828411
DOI https://dx.doi.org/10.2174/1568026053828411 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
subject Index To Volume 2
Current Medicinal Chemistry - Central Nervous System Agents The Insights on Why Diabetes Prevalence May Increase Amid or Post COVID-19 Pandemic
Current Diabetes Reviews Synthesis and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines of thieno[2,3-d]pyrimidine Derivatives Containing Isoxazole Moiety
Letters in Drug Design & Discovery Recent Advances in Pulmonary Hypertension Therapy
Recent Patents on Cardiovascular Drug Discovery β-Carboline Alkaloids: Biochemical and Pharmacological Functions
Current Medicinal Chemistry Synthesis and Antibacterial Evaluation of Model Fluoroquinolone- Benzylidene Barbiturate Hybrids
Letters in Organic Chemistry Discovery of Natural Product Inspired 3-Phenyl-1H-isochromen-1-ones as Highly Potent Antioxidant and Antiplatelet Agents: Design, Synthesis, Biological Evaluation, SAR and <i>In Silico</i> Studies
Current Pharmaceutical Design Withdrawal Notice: Therapeutic Options for Treatment of COVID-19: A Review from Repurposed Drugs to New Drug Targets
Current Drug Targets Oxytocin as a Potential Adjuvant Against COVID-19 Infection
Endocrine, Metabolic & Immune Disorders - Drug Targets Prodrug Design Targeting Intestinal PepT1 for Improved Oral Absorption: Design and Performance
Current Drug Metabolism Liver and COVID-19 - A Review and Clinical Approach
Coronaviruses Artificial Intelligence in Pharmacovigilance and COVID-19
Current Drug Safety Hydrogen Commonly Applicable from Medicine to Agriculture: From Molecular Mechanisms to the Field
Current Pharmaceutical Design Heart Failure in North America
Current Cardiology Reviews Quantitative Structure Activity Relationship (QSAR) Analysis of Substituted 4-Oxothiazolidines and 5-Arylidines as Lipoxygenase Inhibitors
Mini-Reviews in Medicinal Chemistry The Effect of Psychological Stress and Social Isolation on Neuroimmunoendocrine Communication
Current Pharmaceutical Design Ferroptosis Inducers for Prostate Cancer Therapy
Current Medicinal Chemistry Could Targeting HMGB1 be Useful for the Clinical Management of COVID-19 Infection?
Combinatorial Chemistry & High Throughput Screening Exploiting High-Throughput Ion Channel Screening Technologies in Integrated Drug Discovery
Current Pharmaceutical Design Chem-Bioinformatics : Computational Modeling of TIBO Derivatives
Anti-Infective Agents in Medicinal Chemistry