HTS is a high-tech way to hasten the drug discovery process, allowing quick and efficient screening of large compound libraries at a rate of a few thousand compounds per day or per week.
High-throughput screening is a process used in drug discovery to rapidly test large numbers of chemical compounds and substances against a biological target. It allows researchers to quickly screen libraries of tens to hundreds of thousands of potential compounds. The goal is to identify initial 'hits' that show activity against the target. Potential hits are then further tested and refined to identify lead compounds that could progress to drug development. High-throughput screening utilizes microplate technologies, robotics, and automated detection methods to efficiently process many samples in parallel. This process has helped identify numerous potential drug candidates by rapidly evaluating huge numbers of substances for activity.
High-throughput screening is a process used in drug discovery to rapidly test large numbers of chemical compounds and substances against a biological target. It allows researchers to quickly screen millions of potential candidate compounds. The goal is to identify initial "hits" or active compounds that can then be further optimized into potential drug "leads". Key aspects of high-throughput screening include using miniaturized assay plates with many wells, robotics for liquid handling, sensitive detectors to read assay results, and data processing software to analyze large datasets from multiple tests. This allows researchers to potentially screen over 100,000 compounds per day in their search for new medicines.
High-throughput screening (HTS) is a drug discovery process that allows automated testing of large numbers of chemical or biological compounds for a specific biological target. It uses robotic systems to rapidly screen compound libraries in microtiter plates with many wells. This allows identification of hits - compounds that show desired effects on the target. Hits then undergo further testing and optimization to become drug leads. HTS has applications in drug discovery, toxicology studies, and identification of drug-drug interactions. It is an important tool that has increased efficiency in early-stage drug development.
Drug Discovery subject (clinical research)Jannat985397
The document discusses various topics related to drug discovery including methods of target validation, combinatorial chemistry, quantitative structure-activity relationship analysis, and computer-aided drug design. It describes the multi-step process of drug discovery from identifying potential drug targets to optimizing lead compounds and outlines the steps of pre-clinical and clinical drug testing required for regulatory approval. Key aspects covered include high-throughput screening techniques used to identify hits from compound libraries as well as tools for drug design like solid phase synthesis and parallel synthesis.
PHYTOCHEMISTRY.ppt studie exames and preprRabiKhan51
High throughput screening (HTS) is a drug discovery process used in the pharmaceutical industry to rapidly test large numbers of compounds for activity against biological targets. It involves creating a library of compounds, developing miniaturized assays, and automating the screening process using microplates and robotics. The goal is to identify "hits" or compounds that show activity and can be further characterized. HTS of tannins follows a similar systematic approach, sourcing tannin-rich materials, extracting and modifying tannin structures, developing cell-based or enzyme assays, screening the library, and identifying hits that can then be confirmed, characterized, and optimized.
Back Rapid lead compounds discovery through high-throughput screeningrita martin
High-throughput screening process are used by today most of the drug discovery industries, this process helps pharmaceutical researches to make drug discovery process faster and also increase the quality and quantity of drugs production. This process in combination with robotics, data processing and control software, liquid handling devices and sensitive detectors allows a researcher to quickly conduct millions of chemical, genetic or pharmacological tests
- Assay development is the process of creating biological and compound screening assays to identify compounds, called "hits", that have desired activity at drug targets. This involves developing biochemical and cell-based assays.
- Key factors in assay development include relevance, reproducibility, quality as measured by Z'-factor, and avoiding interference. High throughput screening uses automation to test tens of thousands of compounds against targets daily using miniaturized assays.
- Biochemical assays use purified protein or enzyme targets, while cell-based assays examine responses at transcriptional, proliferation, or second messenger levels. Automation and robotics are important for achieving desired screening rates in high throughput screening.
High Throughput Screening (HTS) involves the automated screening of large libraries of chemical compounds against biological targets at a rapid pace. HTS uses robotics, miniaturization, and automation to screen 50,000-100,000 compounds per week. The goals of HTS are to identify compounds that selectively bind and modulate biological targets of interest. Hits identified through primary screening are then evaluated further through secondary assays, SAR analysis, and in vitro/in vivo studies. HTS accelerates drug discovery by allowing for the rapid evaluation of large compound libraries.
High-throughput screening is a process used in drug discovery to rapidly test large numbers of chemical compounds and substances against a biological target. It allows researchers to quickly screen libraries of tens to hundreds of thousands of potential compounds. The goal is to identify initial 'hits' that show activity against the target. Potential hits are then further tested and refined to identify lead compounds that could progress to drug development. High-throughput screening utilizes microplate technologies, robotics, and automated detection methods to efficiently process many samples in parallel. This process has helped identify numerous potential drug candidates by rapidly evaluating huge numbers of substances for activity.
High-throughput screening is a process used in drug discovery to rapidly test large numbers of chemical compounds and substances against a biological target. It allows researchers to quickly screen millions of potential candidate compounds. The goal is to identify initial "hits" or active compounds that can then be further optimized into potential drug "leads". Key aspects of high-throughput screening include using miniaturized assay plates with many wells, robotics for liquid handling, sensitive detectors to read assay results, and data processing software to analyze large datasets from multiple tests. This allows researchers to potentially screen over 100,000 compounds per day in their search for new medicines.
High-throughput screening (HTS) is a drug discovery process that allows automated testing of large numbers of chemical or biological compounds for a specific biological target. It uses robotic systems to rapidly screen compound libraries in microtiter plates with many wells. This allows identification of hits - compounds that show desired effects on the target. Hits then undergo further testing and optimization to become drug leads. HTS has applications in drug discovery, toxicology studies, and identification of drug-drug interactions. It is an important tool that has increased efficiency in early-stage drug development.
Drug Discovery subject (clinical research)Jannat985397
The document discusses various topics related to drug discovery including methods of target validation, combinatorial chemistry, quantitative structure-activity relationship analysis, and computer-aided drug design. It describes the multi-step process of drug discovery from identifying potential drug targets to optimizing lead compounds and outlines the steps of pre-clinical and clinical drug testing required for regulatory approval. Key aspects covered include high-throughput screening techniques used to identify hits from compound libraries as well as tools for drug design like solid phase synthesis and parallel synthesis.
PHYTOCHEMISTRY.ppt studie exames and preprRabiKhan51
High throughput screening (HTS) is a drug discovery process used in the pharmaceutical industry to rapidly test large numbers of compounds for activity against biological targets. It involves creating a library of compounds, developing miniaturized assays, and automating the screening process using microplates and robotics. The goal is to identify "hits" or compounds that show activity and can be further characterized. HTS of tannins follows a similar systematic approach, sourcing tannin-rich materials, extracting and modifying tannin structures, developing cell-based or enzyme assays, screening the library, and identifying hits that can then be confirmed, characterized, and optimized.
Back Rapid lead compounds discovery through high-throughput screeningrita martin
High-throughput screening process are used by today most of the drug discovery industries, this process helps pharmaceutical researches to make drug discovery process faster and also increase the quality and quantity of drugs production. This process in combination with robotics, data processing and control software, liquid handling devices and sensitive detectors allows a researcher to quickly conduct millions of chemical, genetic or pharmacological tests
- Assay development is the process of creating biological and compound screening assays to identify compounds, called "hits", that have desired activity at drug targets. This involves developing biochemical and cell-based assays.
- Key factors in assay development include relevance, reproducibility, quality as measured by Z'-factor, and avoiding interference. High throughput screening uses automation to test tens of thousands of compounds against targets daily using miniaturized assays.
- Biochemical assays use purified protein or enzyme targets, while cell-based assays examine responses at transcriptional, proliferation, or second messenger levels. Automation and robotics are important for achieving desired screening rates in high throughput screening.
High Throughput Screening (HTS) involves the automated screening of large libraries of chemical compounds against biological targets at a rapid pace. HTS uses robotics, miniaturization, and automation to screen 50,000-100,000 compounds per week. The goals of HTS are to identify compounds that selectively bind and modulate biological targets of interest. Hits identified through primary screening are then evaluated further through secondary assays, SAR analysis, and in vitro/in vivo studies. HTS accelerates drug discovery by allowing for the rapid evaluation of large compound libraries.
The high throughput screening is the first step of the docking or computational method of drug discovery. This slide will help you to understand the basic things in HTVS.
High throughput screening is a type of assay. By this assay we can identified the target or binding site of drugs. Its mainly performed during the drug discovery process.
Combinatorial chemistry and high throughput screeningAnji Reddy
Combinatorial chemistry and high-throughput screening techniques allow for the rapid synthesis and testing of large libraries of compounds. Combinatorial chemistry uses solid and solution phase methods to efficiently produce thousands of compounds, while high-throughput screening employs automated instrumentation like microtiter plates to quickly assess large numbers of compounds through functional or non-functional assays. These approaches provide advantages for drug discovery by facilitating the identification of hit compounds for further optimization into drug leads.
CoMPARA: Collaborative Modeling Project for Androgen Receptor ActivityKamel Mansouri
This project used a combination of in vitro high-throughput screening assays and computational models to prioritize over 50,000 chemicals for androgen receptor (AR) activity testing. An international collaboration developed consensus models integrating 11 ToxCast/Tox21 assays which accurately predicted AR agonists and antagonists in a validation set. The resulting data and predictions will be used to select chemicals for further testing by ToxCast/Tox21 and other projects in a fast, cost-effective manner.
This document summarizes progress made and remaining challenges in developing new approach methods for regulatory toxicology assessments. It outlines several new approach methods developed including high-throughput in vitro screening databases and models. However, it notes remaining scientific challenges including limited metabolic and biological complexity of current in vitro assays and gaps in exposure and dosimetry data. The document also discusses philosophical challenges in validating new approach methods, defining adversity at the molecular level, and gaining acceptance for qualitative and quantitative uncertainties compared to traditional animal studies.
This document discusses high-throughput screening (HTS) techniques used in drug discovery. HTS allows for the rapid automated testing of large numbers of chemical compounds. Various detection methods are used in HTS including spectroscopy, chromatography, calorimetry, and microscopy. The document outlines the methodology of HTS, which involves depositing samples and reagents into multi-well plates and monitoring reactions. Cell-based assays are highlighted as being important for HTS as they can provide insights into effects on biological pathways in an environment similar to in vivo conditions.
1. High throughput screening (HTS) is a process for screening large numbers of biological compounds against selected targets using automated equipment. It aims to accelerate the drug discovery process.
2. The key steps in HTS include target identification, reagent preparation, assay development, screening compound libraries, data analysis and management. HTS assays can be biochemical, cellular, or involve measuring second messengers.
3. HTS has various applications in natural product drug discovery, including identifying inhibitors of human thrombin from plant extracts. Euphane triterpenes isolated from Lantana camara leaves showed potent thrombin inhibitory activity.
This document discusses high throughput screening and cell-based assays. It begins by defining high throughput screening as a process used in drug discovery to quickly assay a large number of compounds against a biological target to identify hits or leads. It then describes some key aspects of high throughput screening methodology including detection methods like spectroscopy, chromatography, and microscopy. The document outlines the advantages of cell-based assays compared to biochemical assays, noting they provide a more accurate representation using live cells. Finally, it defines the key elements of a cell-based assay as having a cellular component, a target molecule, an instrument, and informatics for data analysis.
High-throughput screening (HTS) is a scientific method used in drug discovery that allows researchers to quickly test millions of chemical, genetic, or pharmacological compounds using robotics, detectors, and other automated tools. The key tool is a microtiter plate containing hundreds to thousands of wells, each with a different compound. Automated systems transfer plates between stations for mixing, incubation, and analysis to generate large amounts of experimental data. Effective experimental design, quality control, and data analysis methods are needed to identify meaningful results, or "hits", from large HTS datasets. Recent advances allow screening millions of reactions much faster and with less reagent volume than before.
Pre-clinical drug development involves several key stages: high throughput screening to identify potential drug candidates, toxicology studies in animal models to determine safety, pharmacological profiling to understand mechanisms of action, and calculating initial human doses. The overall goals are to obtain sufficient data on safety, tolerability and efficacy to receive regulatory approval from the FDA to begin clinical trials in humans. Pre-clinical studies provide critical data required for an Investigational New Drug (IND) application to the FDA.
Presentation for Texas A&M Superfund Research Center virtual learning series, Big Data in Environmental Science and Toxicology. More details at https://superfund.tamu.edu/big-data-session-2-aug-18-2021/
The document discusses various topics related to drug discovery including target identification and validation, high-throughput screening, hit and lead identification, computational approaches like docking and de novo design, and clinical trial phases. It provides definitions for key terms like target, screening, hit, and lead. It also discusses sources for screening libraries and describes factors to consider for an optimal drug target.
This document provides an overview of high throughput screening (HTS). It defines HTS as a process that can quickly screen 10,000-100,000 compounds per day to identify interactions between chemicals and biological targets. The document outlines the history, definitions, instrumentation, techniques, applications and limitations of HTS. HTS is an important tool in drug discovery for identifying hit compounds from libraries that can then be optimized into lead molecules.
The document discusses various topics related to drug discovery through bioinformatics and computational approaches. It begins by discussing comparative genomics and using knowledge about model organisms to identify similar biological areas and pathways in other species. It also discusses topics like high-throughput screening of large libraries, the definitions of targets, hits and leads in drug discovery, and approaches like using RNAi and phenotypic screening in model organisms. Finally, it discusses computational methods that can be used throughout the drug discovery process, including for target identification and validation, virtual screening, assessing drug-likeness of compounds, and describing compounds using structural and physicochemical descriptors.
The document discusses computer-based drug design and the drug development process. It describes how computational tools can be used in a multidisciplinary approach to increase efficiency, reduce costs and time, and help design drugs to overcome toxic side effects. The key steps in the drug development process are discussed, including target selection, lead discovery through screening compounds and identifying lead molecules, lead optimization to improve properties, and clinical trials. Computational methods like ligand-based and structure-based drug design are used to model potential drug candidates in the goal of developing safe and effective therapeutics.
This document discusses various topics related to drug discovery through bioinformatics. It begins by describing how genome-wide RNAi screening in the nematode C. elegans can be used to identify genes involved in biological pathways related to diseases like type-2 diabetes. It then discusses topics like structural genomics, target identification and validation, high-throughput screening approaches and facilities, sources for screening libraries, criteria for hit and lead compounds, and computational methods used in hit identification and optimization like pharmacophore modeling and evaluating compounds against the "rule of five". Descriptors that can be used for characterizing compounds are also listed.
Drug discovery clinical evaluation of new drugsKedar Bandekar
The document discusses the process of new drug development from initial idea to market launch. It takes 12-15 years and over $1 billion. The process involves identifying a biological target, screening compounds to find hits, optimizing hits to develop leads, and conducting preclinical and clinical trials. Key steps include target identification and validation, high-throughput screening to find initial hits, hit-to-lead and lead optimization processes to improve properties, and three phases of clinical trials to test safety and efficacy in humans. Characteristics of ideal lead compounds include high target affinity and selectivity, drug-like properties, and favorable absorption and toxicity profiles.
Drug discovery clinical evaluation of new drugsKedar Bandekar
The document discusses the process of new drug development from initial idea to market launch. It takes 12-15 years and over $1 billion. The process involves identifying a biological target, screening compounds to find hits, optimizing hits to develop leads, and conducting preclinical and clinical trials. Key steps include target identification and validation, high-throughput screening to find initial hits, hit-to-lead and lead optimization processes to improve properties, and progression through preclinical and clinical phases of drug development. Characteristics of ideal lead compounds include high target affinity and selectivity, efficacy, appropriate physicochemical properties, and favorable ADME profile.
Automation in chemical analysis-need,objectives,instrumentation and process c...GNCO3PushkarBallal
Automation in chemical analysis has significantly advanced over the last few decades through commercial automated analytical systems. These systems provide analytical results with minimal operator intervention. Automation was first applied in clinical laboratories for diagnostic testing but later spread to other industries like process control. Today, many routine and complex analyses are performed using fully or partially automated systems for benefits like reproducibility, increased sample throughput, reduced costs and errors, and meeting regulatory demands. Common automation techniques include discrete sampling instruments that analyze samples sequentially or in parallel and continuous flow systems where samples continuously flow through and are sequentially mixed with reagents.
Microplate Assays and High Throughput Screening HTPCKing Wong
This document discusses microplate assays, which are a key platform for high-throughput screening in biomedical research and pharmacology. Microplates were developed in the 1990s and contain rows and columns of wells in formats of 6, 24, 96, 384, or 1536 wells. They are used for enzyme-linked immunosorbent assays and high-throughput screening of large chemical libraries to identify potential drug candidates. Microplate readers are used to analyze the assays automatedly and efficiently.
Codeless Generative AI Pipelines
(GenAI with Milvus)
https://ml.dssconf.pl/user.html#!/lecture/DSSML24-041a/rate
Discover the potential of real-time streaming in the context of GenAI as we delve into the intricacies of Apache NiFi and its capabilities. Learn how this tool can significantly simplify the data engineering workflow for GenAI applications, allowing you to focus on the creative aspects rather than the technical complexities. I will guide you through practical examples and use cases, showing the impact of automation on prompt building. From data ingestion to transformation and delivery, witness how Apache NiFi streamlines the entire pipeline, ensuring a smooth and hassle-free experience.
Timothy Spann
https://www.youtube.com/@FLaNK-Stack
https://medium.com/@tspann
https://www.datainmotion.dev/
milvus, unstructured data, vector database, zilliz, cloud, vectors, python, deep learning, generative ai, genai, nifi, kafka, flink, streaming, iot, edge
Contenu connexe
Similaire à High Throughput Screening drugg discovery.pdf
The high throughput screening is the first step of the docking or computational method of drug discovery. This slide will help you to understand the basic things in HTVS.
High throughput screening is a type of assay. By this assay we can identified the target or binding site of drugs. Its mainly performed during the drug discovery process.
Combinatorial chemistry and high throughput screeningAnji Reddy
Combinatorial chemistry and high-throughput screening techniques allow for the rapid synthesis and testing of large libraries of compounds. Combinatorial chemistry uses solid and solution phase methods to efficiently produce thousands of compounds, while high-throughput screening employs automated instrumentation like microtiter plates to quickly assess large numbers of compounds through functional or non-functional assays. These approaches provide advantages for drug discovery by facilitating the identification of hit compounds for further optimization into drug leads.
CoMPARA: Collaborative Modeling Project for Androgen Receptor ActivityKamel Mansouri
This project used a combination of in vitro high-throughput screening assays and computational models to prioritize over 50,000 chemicals for androgen receptor (AR) activity testing. An international collaboration developed consensus models integrating 11 ToxCast/Tox21 assays which accurately predicted AR agonists and antagonists in a validation set. The resulting data and predictions will be used to select chemicals for further testing by ToxCast/Tox21 and other projects in a fast, cost-effective manner.
This document summarizes progress made and remaining challenges in developing new approach methods for regulatory toxicology assessments. It outlines several new approach methods developed including high-throughput in vitro screening databases and models. However, it notes remaining scientific challenges including limited metabolic and biological complexity of current in vitro assays and gaps in exposure and dosimetry data. The document also discusses philosophical challenges in validating new approach methods, defining adversity at the molecular level, and gaining acceptance for qualitative and quantitative uncertainties compared to traditional animal studies.
This document discusses high-throughput screening (HTS) techniques used in drug discovery. HTS allows for the rapid automated testing of large numbers of chemical compounds. Various detection methods are used in HTS including spectroscopy, chromatography, calorimetry, and microscopy. The document outlines the methodology of HTS, which involves depositing samples and reagents into multi-well plates and monitoring reactions. Cell-based assays are highlighted as being important for HTS as they can provide insights into effects on biological pathways in an environment similar to in vivo conditions.
1. High throughput screening (HTS) is a process for screening large numbers of biological compounds against selected targets using automated equipment. It aims to accelerate the drug discovery process.
2. The key steps in HTS include target identification, reagent preparation, assay development, screening compound libraries, data analysis and management. HTS assays can be biochemical, cellular, or involve measuring second messengers.
3. HTS has various applications in natural product drug discovery, including identifying inhibitors of human thrombin from plant extracts. Euphane triterpenes isolated from Lantana camara leaves showed potent thrombin inhibitory activity.
This document discusses high throughput screening and cell-based assays. It begins by defining high throughput screening as a process used in drug discovery to quickly assay a large number of compounds against a biological target to identify hits or leads. It then describes some key aspects of high throughput screening methodology including detection methods like spectroscopy, chromatography, and microscopy. The document outlines the advantages of cell-based assays compared to biochemical assays, noting they provide a more accurate representation using live cells. Finally, it defines the key elements of a cell-based assay as having a cellular component, a target molecule, an instrument, and informatics for data analysis.
High-throughput screening (HTS) is a scientific method used in drug discovery that allows researchers to quickly test millions of chemical, genetic, or pharmacological compounds using robotics, detectors, and other automated tools. The key tool is a microtiter plate containing hundreds to thousands of wells, each with a different compound. Automated systems transfer plates between stations for mixing, incubation, and analysis to generate large amounts of experimental data. Effective experimental design, quality control, and data analysis methods are needed to identify meaningful results, or "hits", from large HTS datasets. Recent advances allow screening millions of reactions much faster and with less reagent volume than before.
Pre-clinical drug development involves several key stages: high throughput screening to identify potential drug candidates, toxicology studies in animal models to determine safety, pharmacological profiling to understand mechanisms of action, and calculating initial human doses. The overall goals are to obtain sufficient data on safety, tolerability and efficacy to receive regulatory approval from the FDA to begin clinical trials in humans. Pre-clinical studies provide critical data required for an Investigational New Drug (IND) application to the FDA.
Presentation for Texas A&M Superfund Research Center virtual learning series, Big Data in Environmental Science and Toxicology. More details at https://superfund.tamu.edu/big-data-session-2-aug-18-2021/
The document discusses various topics related to drug discovery including target identification and validation, high-throughput screening, hit and lead identification, computational approaches like docking and de novo design, and clinical trial phases. It provides definitions for key terms like target, screening, hit, and lead. It also discusses sources for screening libraries and describes factors to consider for an optimal drug target.
This document provides an overview of high throughput screening (HTS). It defines HTS as a process that can quickly screen 10,000-100,000 compounds per day to identify interactions between chemicals and biological targets. The document outlines the history, definitions, instrumentation, techniques, applications and limitations of HTS. HTS is an important tool in drug discovery for identifying hit compounds from libraries that can then be optimized into lead molecules.
The document discusses various topics related to drug discovery through bioinformatics and computational approaches. It begins by discussing comparative genomics and using knowledge about model organisms to identify similar biological areas and pathways in other species. It also discusses topics like high-throughput screening of large libraries, the definitions of targets, hits and leads in drug discovery, and approaches like using RNAi and phenotypic screening in model organisms. Finally, it discusses computational methods that can be used throughout the drug discovery process, including for target identification and validation, virtual screening, assessing drug-likeness of compounds, and describing compounds using structural and physicochemical descriptors.
The document discusses computer-based drug design and the drug development process. It describes how computational tools can be used in a multidisciplinary approach to increase efficiency, reduce costs and time, and help design drugs to overcome toxic side effects. The key steps in the drug development process are discussed, including target selection, lead discovery through screening compounds and identifying lead molecules, lead optimization to improve properties, and clinical trials. Computational methods like ligand-based and structure-based drug design are used to model potential drug candidates in the goal of developing safe and effective therapeutics.
This document discusses various topics related to drug discovery through bioinformatics. It begins by describing how genome-wide RNAi screening in the nematode C. elegans can be used to identify genes involved in biological pathways related to diseases like type-2 diabetes. It then discusses topics like structural genomics, target identification and validation, high-throughput screening approaches and facilities, sources for screening libraries, criteria for hit and lead compounds, and computational methods used in hit identification and optimization like pharmacophore modeling and evaluating compounds against the "rule of five". Descriptors that can be used for characterizing compounds are also listed.
Drug discovery clinical evaluation of new drugsKedar Bandekar
The document discusses the process of new drug development from initial idea to market launch. It takes 12-15 years and over $1 billion. The process involves identifying a biological target, screening compounds to find hits, optimizing hits to develop leads, and conducting preclinical and clinical trials. Key steps include target identification and validation, high-throughput screening to find initial hits, hit-to-lead and lead optimization processes to improve properties, and three phases of clinical trials to test safety and efficacy in humans. Characteristics of ideal lead compounds include high target affinity and selectivity, drug-like properties, and favorable absorption and toxicity profiles.
Drug discovery clinical evaluation of new drugsKedar Bandekar
The document discusses the process of new drug development from initial idea to market launch. It takes 12-15 years and over $1 billion. The process involves identifying a biological target, screening compounds to find hits, optimizing hits to develop leads, and conducting preclinical and clinical trials. Key steps include target identification and validation, high-throughput screening to find initial hits, hit-to-lead and lead optimization processes to improve properties, and progression through preclinical and clinical phases of drug development. Characteristics of ideal lead compounds include high target affinity and selectivity, efficacy, appropriate physicochemical properties, and favorable ADME profile.
Automation in chemical analysis-need,objectives,instrumentation and process c...GNCO3PushkarBallal
Automation in chemical analysis has significantly advanced over the last few decades through commercial automated analytical systems. These systems provide analytical results with minimal operator intervention. Automation was first applied in clinical laboratories for diagnostic testing but later spread to other industries like process control. Today, many routine and complex analyses are performed using fully or partially automated systems for benefits like reproducibility, increased sample throughput, reduced costs and errors, and meeting regulatory demands. Common automation techniques include discrete sampling instruments that analyze samples sequentially or in parallel and continuous flow systems where samples continuously flow through and are sequentially mixed with reagents.
Microplate Assays and High Throughput Screening HTPCKing Wong
This document discusses microplate assays, which are a key platform for high-throughput screening in biomedical research and pharmacology. Microplates were developed in the 1990s and contain rows and columns of wells in formats of 6, 24, 96, 384, or 1536 wells. They are used for enzyme-linked immunosorbent assays and high-throughput screening of large chemical libraries to identify potential drug candidates. Microplate readers are used to analyze the assays automatedly and efficiently.
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https://ml.dssconf.pl/user.html#!/lecture/DSSML24-041a/rate
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2. Commonly used terms in drug discovery
• High throughput screen: an optimized, miniaturized assay format that enables the testing of >
100,000 chemically diverse compounds per day.
• Assay: a test system in which biological activity can be detected
• Hit: a molecule with confirmed concentration-dependent activity in a screen, and known chemical
structure. The output of most screens
• Progressible hit: a representative of a compound series with activity via acceptable mechanism of
action and some limited structure-activity relationship information
• Lead: a compound with potential (as measured by potency, selectivity, physico-chemical properties,
absence of toxicity or novelty) to progress to a full drug development programme
6. Drug Discovery Process:
•The key steps of drug discovery are:
•Research – it takes average 2 to 3 years
•Pre-clinical testing - average 1 year
•Clinical trial testing (involving human
patients) - average 10 years
•Regulatory approval - average 2 years
7. High-throughput screening (HTS)
• High throughput screening (HTS) is the use of automated equipment to rapidly test
thousands to millions of samples for biological activity at the model organism, cellular,
pathway, or molecular level.
• HTS can identify active compounds, antibodies, genes, or one or more candidates
based on specific criteria.
• HTS uses robotics, data processing/control software, liquid handling devices, and
sensitive detectors to quickly conduct millions of chemical, genetic, or pharmacological
tests.
• It allows automation to quickly assay the biological or biochemical activity of a large
number of compounds.
• It is a useful for discovering ligands for receptors, enzymes, ion channels or other
pharmacological targets, or pharmacologically profiling a cellular or biochemical
pathway of interest
• It is a drug-discovery process widely used in the pharmaceutical industry.
8.
9. ❑ Steps in the HTS
• 1st stage screening
o To Test the optical clarity, abrasion resistance, and adhesion
o It Eliminates ~90% of samples
• 2nd stage screening
o It Test whether the ability, integrity, gloss, and surface smoothness
o It eliminates the ~10% of the samples
• There are 4 steps in HTS
o Preparation of samples and compound libraries
o Establishment of a method suitable for lab automation
o Configuration of a robotic workstation
o Acquisition and handling of data
10. ❑Elements of the HTS: -
1) Chemical compound libraries: - this comprises the database of a samples that
are reacted with the target molecules. Typical libraries might include a range
of proteins or genes.
2) Suitable assay method: - this must me easy to replicate and suitable for
automated.
3) Robotic system: - it carries out all the automated process, it add the target
compound and wells, prepare the plates, add the reagents, set the reaction
conditions and prepare the samples for measurement.
4) Data anaylis system: - it takes all the results generated from the assays and
screens them for positive hits.
11. ❑ Types of HTS: -
❑ The most widely used HTS techniques for PPIs include the: -
• two-hybrid assay
• affinity purification
• fluorescence polarization (FP)
• fluorescence resonance energy transfer (FRET).
❑ Types of high throughput assays: -
• Homogeneous assay
• Heterogeneous assays
• Biochemical assays
• Applications
12. • Genomics: - it is a Core Facility provides technical, instrument, and
professional development and next generation sequencing, gene
expression services, flow cytometry
• Protein Analysis: - a protein high throughput formulation (HTF)
platform is based on the use of microplates.
• DNA Sequencing: - it refers to the amount of DNA molecules read at
the same time. Technologies are now capable of sequencing many
fragments of DNA in parallel. This enables scientists to read hundreds
of millions of DNA fragments and generate more data, with less time
and costs than ever before.
• High-throughput technology can also be put to use in other areas
besides drug development.
13.
14. Detection method in HTS
• Spectroscopy: - It is used as a tool for studying the structures of atoms and molecules
• Mass spectrometry: - it also called mass spectroscopy, analytic technique by which
chemical substances are identified by the sorting of gaseous ions in electric and
magnetic fields according to their mass-to-charge ratios.
• Chromatography:- it is a technique for separating the components, or solutes, of a
mixture on the basis of the relative amounts of each solute.
• Calorimetry: - it enables the continuous monitoring of samples for a prolonged period.
• X ray diffraction: it powders diffraction (XRD) is a rapid analytical technique primarily
used for phase identification of a crystalline material and can provide information on
unit cell dimensions
• Microscopy: - it is a technical field of using microscopes to view samples & objects that
cannot be seen with the unaided eye.
• Radioactive methods: -Radioactive methods of analysis are particularly useful for the
detection and determination of trace quantities of materials and for the measurement
of larger quantities in complicated systems.
15.
16.
17. History
• HTS was invented by Dr Gyula Takatsky in 1951, who machined 6
rows of 12 wells in Lucite to make the first microtiter plate.
• The microtiter plate has further grown to include standardized 96,
384, 1536 well formats, with additional 3072 well nanoplate
formats.
• “twenty eight plates are currently run daily on the Accuri C6 Hyper
Cytometer combination. We could run up to 40 plates in a standard
8 hour workday, over 12,000 comp
20. •High throughput screening
for drug discovery
•Why High throughput screening need arises ?
•FACT 1: recent understanding of disease mechanisms has
dramatically increased no. of protein targets for new drug treatment
•FACT 2: new technologies have increased the no. of drugs that can
be tested for activity at these targets.
21. ❑ Goals of HTS
❑ The primary goal of HTS is to identify through compound library
screenings, candidates that affect the target in the desired way, so-called
“hits” or “leads”.
❑ This is usually achieved employing liquid handling devices, robotics, plate
readers as detectors, and dedicated software for instrumentation control
and data processing.
❑ HTS screen about 50,000 – 100,000 compounds per day
22.
23. Explanation
• High-throughput screening is a method for scientific experimentation especially
used in drug discovery and is relevant to biology and chemistry. This process in
combination with robotics, data processing and control software, liquid
handling devices and sensitive detectors allows a researcher to quickly conduct
millions of chemical, genetic or pharmacological tests.
• High-throughput screening can rapidly identify active compounds, antibodies or
genes which modulate a particular bimolecular pathway. It can be considered -
a process in which batches of compounds are tested for binding activity or
biological activity against target molecules.
• High-throughput screening is a process of screening more compounds against
more targets per unit time, which should generate more hits, which in turn will
generate more leads, subsequently generating more products.
• Various technologies like high-throughput screening defined by the number of
compounds tested to be in the range of 10,000-100,000 per day, ultra high-
throughput screening is defined by screening more than 100,000 data point
generated per day. These two technologies play a vital role in drug discovery to
find new chemical compounds.
24.
25.
26.
27. Which strategy is best for hit identification?
➢ When a target is identified, a decision has to be made about which chemicals to
screen, in order to identify potential lead compounds.
➢ There are two types of strategies best for hit identification
• Random screening :
o All possible drug molecules screened against target. This is simply not possible.
• Focussed screening :
o A limited number of compounds are pre-selected for screening.
Has proved successful as a hit generation strategy.
Useful when 3D structure of target is known (e.g. crystal structure of a receptor)
28. ❑ Procedure: -
• High-throughput screening in drug discovery is used to screen :
• Novel biological active compounds
• Natural products
• Combinatorial libraries (Ex: peptides; chemicals)
• Biological libraries
• DNA chips
• RNA chips
• Protein chips
• Modern microplates for high-throughput screening assays are
performed in automation-friendly microtiter plates with a 96, 384,
1536 or 3456 well format.
• These wells contain experimentally useful matter, often an aqueous
solution of dimethyl sulfoxide (DMSO).
29. • For most drug discovery labs, the library collection has grown from
400,000 to 1 million or more compounds. The standard paradigms
used to screen these libraries have evolved to automated 384 wells or
higher density single compound test formats.
• Primary screen is designed to rapidly identify hits from compound
libraries. The goals are to minimize the number of false positives and
maximize the number of confirmed hits.
• Depending on the assay, hit rates typically range between 0.1 – 5 per
cent. This number also depends on the cutoff parameters set by the
researchers, as well as the dynamic range of a given assay.
• Primary screens are run in multiplets of single compound
concentrations. Hits are then retested, usually independently from the
first assay.
30. • If a compound exhibits the same activity, it is coined as confirmed hit, which
proceeds to secondary screens or lead optimization. The results from lead
optimization are used to decide which substances will make it on to clinical
trials.
• In combination with bioinformatics, it allows potential drugs to be quickly and
efficiently screened to find candidates that should be explored in more detail.
Initial screening of these compounds for their binding ability is the job for high-
throughput screening.
• The key to high-throughput screening is to develop a test, or assay, in which
binding between a compound and a protein causes some visible change that
can be automatically read by a sensor. Typically the change is emission of light
by a fluorophore in the reaction mixture.
• One way to make this occur is to attach the fluorophore to the target protein in
such a way that its ability to fluoresce is diminished (quenched) when the
protein binds to another molecule. A different system measures the difference
in a particular property of light (polarization) emitted by bound versus unbound
fluorophores. Bound fluorophores are more highly polarized and this can be
detected by sensors.
31. ❑ Procedure: -
• The sets of compounds produced by combinatorial chemistry are generally referred
to as libraries, which depending on how the solid- phase is handled, may be either
mixtures or individual compounds.
• There are a range of options for testing the libraries in a biological assay.
o Test mixture in solution
o Test individual compounds in solution Test compounds on the beads
32. Test mixture in solution :
• All the compounds are cleaved from the beads and tested in solution.
• If activity in a pharmacological screen is observed,
it is difficult to find out which compounds are active. To identify the
most active component, it is necessary to resynthesize the
compounds individually and thereby find the most potent. This
iterative process of resynthesis and screening is one of the most
simple and successful methods for identifying active compounds
from libraries.
33. Test individual compounds in solution
• A second method is to separate the beads manually into
individual wells and cleave the compounds from the solid-phase.
These compounds can now be tested as individual entities.
•Test compounds on the beads :
• A third method for screening is testing on the beads, using a
colorimetric or fluorescent assay technique. If there are active
compounds, the appropriate beads can be selected by color or
fluorescence.
34. Chromatography
• Chromatography (from Greek word ‘chroma’ a “color” and ‘graphic’ to “write”)
chroma mans a color and graphic means to write.
• It is the collection term for a set of laboratory techniques for the separation of
mixtures.
• The mixture is dissolved in a fluid called the mobile phase, which carries it
through a structure holding another material called the stationary phase.
• The various constituents of the mixture travel at it different speed causing them
to separate.
• The separation is based on differential partitioning between the mobile and
stationary phase.
35. ➢ Stationary phase: -
• Stationary phase in chromatography is the one which does not move with the sample
whereas mobile phase in chromatography is one which moves with the sample.
• The stationary phase is polar, usually using silica.
• The stationary phase is composed of either a solid or liquid substance attached to a
glass or a metal surface.
➢ Mobile phase: -
• In chromatography, the mobile phase is a liquid or gas that flows through a
chromatographic column.
• The mobile phase carries the components of a mixture with it, and different
components travel at different rates.
• The mobile phase can be:
o A liquid solvent or mixture of solvents
o A chemically inert gas
o A liquid phase coated on the surface of a solid phase
36. History of chromatography
• It was first employed by the Russian Italian botanist scientists (Mikhail Tsvet) in 1900.
• He continuous to work in the chromatography in the first decade of the 20th century
,primarily for the separation of plant pigment such a ‘chlorophyll’ (which is green) and
‘carotenoids’ (which are orange and yellow).
• The new forms of chromatography developed in the 1930s and 1940s made the technique
useful for a wide range of separation processes and chemical analysis tasks, especially in
biochemistry.
➢ Uses: -
• Chromatography is a method that is used in laboratories for the separation of a mixture. It
is used to test drug levels and water purity.
• It is also used to determine the nutritional value of the food sample.
• It is used to determine the type of chlorophyll in various photosynthetic organisms.
• Pharmaceuticals: Used to analyze components in water, raw materials, and products
• Food and beverage: Used for food and beverage testing
• Molecular biology: Used for DNA fingerprinting and bioinformatics
• Drug testing: Used for drug testing
• Forensics: Used for evidence analysis
37. ➢ Principles: -
• Chromatography is usually consists of a mobile phase and stationary phase.
• Chromatography can be used for the purification or analysis of components from a mixture,
including simple and complex molecules.
• The interaction between the mobile and stationary phase results in the separation of a
compounds from a mixture.
• Different types of chromatographic techniques, such as liquid chromatography (LC), are used
for the separation of proteins.
➢ Applications: -
• Separation:- Chromatography can separate different colors of ink, amino acids, proteins, and
more
• Identification:- Chromatography can identify and separate preservatives and additives in
food
• DNA fingerprinting:- Chromatography can be used in DNA fingerprinting and bioinformatics
• Ion exchange: -Ion exchange chromatography can separate organic and inorganic ions from
an aqueous solution
• Affinity:-Affinity chromatography separates a sample based on its molecular bonds
38. ➢ Types of chromatography: -
• There are several types of chromatography are: -
1. Paper chromatography
2. Thin layer chromatography
3. High - performance liquid chromatography
4. Column chromatography
5. Ion exchange chromatography
6. Gas liquid chromatography
7. Gel chromatography
8. Affinity chromatography
39. 1. Paper chromatography: - it is an analytical chemistry technique that separates
dissolved chemical substances based on their migration rates across sheets of paper.
2. Thin-layer chromatography (TLC): - it is a technique used to separate mixtures of
compounds based on differences in polarity.
3. High-performance liquid chromatography (HPLC) : - it is an analytical technique used
in analytical chemistry and biochemistry to separate, identify, and quantify
components in a mixture.
4. Column chromatography: - it is a separation technique used to isolate compounds
from complex mixtures.
5. Ion exchange chromatography: - Ion exchange chromatography (IEC) is a technique
for separating compounds based on their net charge
6. Gas–liquid chromatography (GLC): - it is a commonly used method for lipid analysis.
7. Gel chromatography: - it is a technique in analytical chemistry that separates
chemical substances by how quickly they pass through a porous, semisolid substance.
Also known as gel filtration
8. Affinity chromatography: - it is a liquid chromatographic method that separates a
biomolecule from a mixture.
40. 1. Paper chromatography: - it is an analytical chemistry technique that separates dissolved
chemical substances based on their migration rates across sheets of paper.
➢ Principle of Paper chromatography: -
• Paper chromatography is of two types based on two different principles.
• The first is the paper adsorption chromatography that is based on the varying degree of
interaction between the molecules and the stationary phase.
• The second type of paper chromatography is the paper partition chromatography.
• It is based on the principle that the moisture on the cellulose paper acts as a stationary
phase for the molecules moving with the mobile phase.
➢ Steps of Paper chromatography: -
• The stationary phase is selected as a fine quality cellulosic paper.
• Different combinations of organic and inorganic solvents are taken as the mobile phase.
• The sample loaded paper is then carefully dipped into the mobile phase not more than
the height of 1 cm
• After the mobile phase reaches near the edge of the paper, the paper is taken out.
41. ➢ Uses of Paper chromatography: -
• Paper chromatography is performed to detect the purity of various pharmaceutical
products.
• It can also be employed to detect contamination in various samples, like food and
beverages.
• This method can also be used for the separation of impurities from various industrial
products.
2. Thin-layer chromatography (TLC): -
• it is a technique used to separate mixtures of compounds based on differences in polarity.
• It's a widely used separation technique for quantitative and qualitative analysis.
➢ Principle of Thin-layer chromatography (TLC): -
• The substrate/ ligand is bound to the stationary phase so that the reactive sites for the
binding of components are exposed.
• After separation, the molecules are seen as spots at a different location throughout the
stationary phase.
• The detection of molecules is performed by various techniques.
42. ➢ Steps of Thin-layer chromatography (TLC): -
• The stationary phase is uniformly applied on the solid support (glass, thin plate or
aluminum foil) and dried.
• The sample is injected as spots on the stationary phase about 1 cm above the edge of
the plate.
• The sample loaded plate is then carefully dipped into the mobile phase not more than
the height of 1 cm.
➢ Uses of Thin-layer chromatography (TLC): -
• Thin-layer chromatography is routinely performed in laboratories to identify different
substances present in a mixture.
• This technique helps in the analysis of fibers in forensics.
• TLC also allows the assay of various pharmaceutical products.
43. 3. High-performance liquid chromatography (HPLC): -
• High-performance liquid chromatography (HPLC) is an analytical technique used in
analytical chemistry and biochemistry to separate, identify, and quantify components in
a mixture.
• It was first discovered in the early twentieth century and was initially used to separate
colored compounds.
➢ Principle of HPLC: -
• The molecules having higher affinity remain adsorbed for a longer time decreasing their
speed of movement through the column.
• However, the molecules with lower affinity move with a faster movement, thus allowing
the molecules to be separated in different fractions.
➢ Steps of HPLC
• The column is prepared by taking a glass tube that is dried and coated with a thin,
uniform layer of stationary phase (cellulose, silica).
• The mobile phase then moves down to a detector that detects molecules at a certain
absorbance wavelength.
• The separated molecules can further be analyzed for various purposes.
44. ➢ Uses of HPLC
• High-performance liquid chromatography is used in the analysis of pollutants present
in environmental samples.
• It is performed to maintain product purity and quality control of various industrial
productions.
• This technique can also be used to separate different biological molecules like
proteins and nucleic acids.
❑ Formula (reflective formula) paper chromatography
RF = distance travelled by the substance
distance travelled by the solvent
• The RF value helps for the identification of unknown
45. Characteristics and properties of therapeutic area
• A therapeutic target is a biological molecule, biological pathway, or physio local response
that is associated with a particular disease process.
• It may be inhibited or activated by a therapy in a way that will change the course of the
disease in a positive way.
• Therapeutic area mean, the grouping of similar diseases 0or conditions under a
generalized heading.
• E.g.- oncology
- cardiology
- dermatology
- neurology
- hematology
• These therapeutic areas guide the efforts of researchers, physicians and pharmaceutical
companies in their pursuit of better healthcare solutions.
➢ Cardiovascular (heart disease)
• The heart disease describes a range of conditions that affect the heart
- blood vessels disease
- irregular heartbeats (arrythmia)
- heart problems (congenital heart defects)
- disease of the heart muscle
- heart valve disease
46. ➢ Symptoms: -
• Angina or chest pain
• Difficulty in breathing
• Fatigue
• Swelling due to fluid retention or edema
➢ Causes: -
• Damage to all or parts of the heart
• A low supply of oxygen and nutrients to heart
• The rhythm of the heart
➢ Risk factors: -
• High blood pressure (BP)
• High cholesterol
• Smoking
• A high intake of alcohol
• Diabetes
• Sleep apnea
48. • The patient should be the primary focus of interaction
• A professional attitude sets the tone of the therapeutic relationship
• Use self-disclosure cautiously & only when it has a therapeutic purpose
• Avoid social relationship with patients & maintain confidently
• Implement interventions on theoretical basis
• Guide the patient to reinterpret his or her experience rationally
Characteristics of therapeutic area
49. Question bank
1. Write the relationship between drug targets and therapeutic drugs?
• The protein molecules are the primary target of drug molecules.
• Molecular biology is providing new insights into the nature of genes, proteins and the
relationship between them.
• Whereas the time-honored biochemical and physiological approaches can show how
disease affects function at the level of cells, tissues, organs and individuals.
• The links between the two nevertheless remain tenuous, fact which greatly limits our
ability to relate drug targets to therapeutic effects.
2. Write a short note on therapeutic targets?
• A therapeutic target is a biological molecule, biological pathway, or physio local response
that is associated with a particular disease process.
• It may be inhibited or activated by a therapy in a way that will change the course of the
disease in a positive way.
• Therapeutic targets are used to screen potential therapies in the discovery phase of the
therapy development process.
• the pathway information and the corresponding drugs/ligands directed at each of these
targets.
• Pharmaceutical agents generally exert their therapeutic effect by binding to a particular
protein or nucleic acid target
50. 3. Write advantages and disadvantages of a small molecule drug?
❑ Advantages: -
• ‘Chemical space’ is so vast that synthetic chemicals according to many experts, it have the
potential for a right molecule exists: it is just a matter of finding it.
• Doctors and patients are thoroughly familiar with conventional drugs as medicines, and
the many different routes of administration that are available.
• Clinical pharmacology in its broadest sense has become part of the knowledge base of
every practicing doctor and indeed part of everyday culture.
• Oral administration is often possible, as well as other routes where appropriates.
❑ Disadvantages: -
• Side and effects and toxicity remain a serious and unpredictable problem.
• It causing failures in late development, or even after registration.
• Humans and other animals have highly developed mechanism for eliminating foreign
molecules.
• The drug design often has to contend with pharmacokinetic problems.
• Oral administration is poor for many compounds and peptides cannot be given orally.
51. 4. write a short notes on conventional therapeutic drugs?
• The conventional drug design methods include random screening of chemicals found in
nature or synthesized in laboratories.
• The time consuming is 10 – 15 years and it is very expensive.
• Small-molecule drugs, either synthetic compounds or natural products have for long
bene the mainstay of therapeutics.
• The pre-eminent role of conventional small-molecule drugs may decline as
biopharmaceutical products Grow in importance
• The drugs delivery system will allow the drugs to act much more selectivity where they
are needed, and thus reduce the burden of side effects.