Publications associées à Hit to lead

Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry

Libraries of DNA-Encoded small molecules created using combinatorial chemistry and synthetic oligonucleotides are being applied to drug discovery projects across the pharmaceutical industry. The majority of reported projects describe the discovery of rever ...

PERGAMON-ELSEVIER SCIENCE LTD2021

Miniaturized technologies for high-throughput drug screening enzymatic assays and diagnostics - A review

Paul Joseph Dyson, Sarah Alexandra Pais Pereira

Drug discovery is a complex, multistep process, in which many challenges need to be overcome at each stage, from the discovery of a biomolecular target to the ensuring of the efficacy and safety of a compound in humans. Today's analytical methods allow ten ...

ELSEVIER SCI LTD2020

Multidisciplinary Preclinical Investigations on Three Oxamniquine Analogues as New Drug Candidates for Schistosomiasis

Ursula Röthlisberger, François Louis Mouvet

Schistosomiasis is a disease of poverty affecting millions of people. Praziquantel (PZQ), with its strengths and weaknesses, is the only treatment available. We previously reported findings on three lead compounds derived from oxamniquine (OXA), an old ant ...

WILEY-V C H VERLAG GMBH2020

Extrapolating the Fragment-Based Approach to Inorganic Drug Discovery

Paul Joseph Dyson, Lucinda Kate Batchelor

The fragment-based approach is a well-established strategy for organic drug discovery. Recent studies have shown that this approach also has considerable potential in medicinal inorganic chemistry, and yet the approach has not been formally described. Here ...

ELSEVIER2019

Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators

Gerardo Turcatti, Benjamin Rappaz, Fabien Kuttler, Damiano Banfi, Pierre Marquet, Pascal Jourdain

The ionotropic GABA(A) receptors represent the main target for different groups of widely used drugs having hypnotic and anxiolytic effects. So far, most approaches used to assess GABA activity involve invasive low -throughput electrophysiological techniqu ...

2019

A Universal Assay for Aminopeptidase Activity and Its Application for Dipeptidyl Peptidase-4 Drug Discovery

Gerardo Turcatti, Marc Chambon, Julien Bortoli Chapalay, Elena Goun, Jonathan Patrice Vesin, Arkadiy Bazhin, James William Collins

Aminopeptidases, such as dipeptidyl peptidase 4 (DPP-4, CD26), are potent therapeutic targets for pharmacological interventions because they play key roles in many important pathological pathways. To analyze amino-peptidase activity in vitro (including hig ...

AMER CHEMICAL SOC2019

Advancing Drug Discovery via Artificial Intelligence

Horst Vogel, Thamani Dahoun, Shuguang Yuan

Drug discovery and development are among the most important translational science activities that contribute to human health and wellbeing. However, the development of a new drug is a very complex, expensive, and long process which typically costs 2.6 bill ...

ELSEVIER SCIENCE LONDON2019

An optimized and validated 384-well plate assay to test platelet function in a high-throughput screening format

Nikolaos Stergiopoulos, Olivier Burri, Marc Chambon, Julien Bortoli Chapalay, Fabiana Pereira Da Costa Fraga, Augusto Martins Lima, Maiia Bragina

Despite significant advances in the treatment of cardiovascular diseases, antiplatelet therapies are still associated with a high risk of hemorrhage. In order to develop new drugs, methods to measure platelet function must be adapted for the high-throughpu ...

TAYLOR & FRANCIS INC2019

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Hit to lead

Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry

Miniaturized technologies for high-throughput drug screening enzymatic assays and diagnostics - A review

Multidisciplinary Preclinical Investigations on Three Oxamniquine Analogues as New Drug Candidates for Schistosomiasis

A scalable CRISPR/Cas9-based fluorescent reporter assay to study DNA double-strand break repair choice

Design and validation of bioorthogonal probes for cellular disease models

Extrapolating the Fragment-Based Approach to Inorganic Drug Discovery

Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators

A Universal Assay for Aminopeptidase Activity and Its Application for Dipeptidyl Peptidase-4 Drug Discovery

Advancing Drug Discovery via Artificial Intelligence

An optimized and validated 384-well plate assay to test platelet function in a high-throughput screening format

Graph Chatbot

Chattez avec Graph Search

Extrapolating the Fragment-Based Approach to Inorganic Drug Discovery

Miniaturized technologies for high-throughput drug screening enzymatic assays and diagnostics - A review

Multidisciplinary Preclinical Investigations on Three Oxamniquine Analogues as New Drug Candidates for Schistosomiasis

A Universal Assay for Aminopeptidase Activity and Its Application for Dipeptidyl Peptidase-4 Drug Discovery

Advancing Drug Discovery via Artificial Intelligence

Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry

An optimized and validated 384-well plate assay to test platelet function in a high-throughput screening format

A scalable CRISPR/Cas9-based fluorescent reporter assay to study DNA double-strand break repair choice

Design and validation of bioorthogonal probes for cellular disease models

Image-Based Marker-Free Screening of GABA(A) Agonists, Antagonists, and Modulators