This document provides an introduction to quantitative structure-activity relationships (QSAR). It defines QSAR as quantifying physicochemical properties of drugs to see their effect on biological activity. Graphs are used to plot activity versus properties, and regression analysis determines correlation. Key properties discussed are hydrophobicity, steric effects, and electronic effects. Hansch analysis uses equations to relate activity to multiple properties. Advantages are understanding structure-activity and enabling novel analog design. Limitations include potential for false correlations and need for large, high-quality datasets.
Commonly used instruments in experimental pharmacologyShaikh Abusufyan
For all YouTube Live video practical series of experimental Pharmacology click:
https://youtube.com/playlist?list=PLBVbJ9HCa1Ba6WSJjeBaK0HMF79hdad3g
For More Such Learning You Can Subscribe to
My YouTube Channel:
https://www.youtube.com/channel/UC5o-WkzmDJaF7udyAP2jtgw/featured?sub_confirmation=1
Facebook Page: https://www.facebook.com/asacademylearningforever
Website Blog: https://itasacademy.blogspot.com/
Antiallergic activity by mast cell stabilization assayHimikaRathi
This document describes procedures for evaluating the antiallergic and mast cell stabilizing activity of drugs. It involves using guinea pigs to test if drugs can prevent bronchoconstriction induced by histamine aerosol exposure. It also involves collecting mast cells from rat peritoneal fluid and observing if drugs can prevent degranulation when exposed to egg albumin. The procedures provide a way to test if drugs can stabilize mast cell membranes and prevent the release of inflammatory mediators associated with allergic responses.
This document discusses QSAR (quantitative structure-activity relationship), which is a mathematical model that relates biological activity to physicochemical properties of molecules. QSAR can be used to predict activity of new compounds. Key parameters used in QSAR include hydrophobicity (measured by partition coefficient), electronic effects (Hammett constant), and steric effects (Taft's steric factor). These parameters influence drug absorption, distribution, and interactions with receptors. QSAR models take the form of biological activity = function(parameters) to develop relationships between activity and molecular properties.
This document presents information on parasympathomimetics, which are drugs that mimic the effects of parasympathetic nervous system stimulation. It discusses how parasympathomimetics can directly activate cholinergic receptors through agonists like acetylcholine, muscarine, and pilocarpine. It also describes how anticholinesterase drugs inhibit the acetylcholinesterase enzyme, increasing the availability of acetylcholine at cholinergic synapses. Specific parasympathomimetic drugs discussed include bethanechol, carbachol, pilocarpine, and echothiophate. The document provides details on the mechanisms of action and therapeutic uses of these cholinergic drugs.
SAR versus QSAR, History and development of QSAR, Types of physicochemical
parameters, experimental and theoretical approaches for the determination of
physicochemical parameters such as Partition coefficient, Hammet’s substituent
constant and Taft’s steric constant. Hansch analysis, Free Wilson analysis, 3D-QSAR
approaches like COMFA and COMSIA.
Herbs, Herbal Drugs
Present Scope of Herbal Drug Industry
Scope of Herbal Drug Medicine and Industry
Indian Herbal Industry
International Scope of Herbal Medicines
World Wide Herbal Trade
Overview on plant based industries and research institutions in India
List of few herbal drug industries in India
List of few herbal research institution/ centres in India
General Introduction to Herbal Industry
Herbal drugs industry: Present scope and future prospects.
A brief account of plant based industries and institutions involved in work on medicinal and
aromatic plants in India.
This document provides an introduction to quantitative structure-activity relationships (QSAR). It defines QSAR as quantifying physicochemical properties of drugs to see their effect on biological activity. Graphs are used to plot activity versus properties, and regression analysis determines correlation. Key properties discussed are hydrophobicity, steric effects, and electronic effects. Hansch analysis uses equations to relate activity to multiple properties. Advantages are understanding structure-activity and enabling novel analog design. Limitations include potential for false correlations and need for large, high-quality datasets.
Commonly used instruments in experimental pharmacologyShaikh Abusufyan
For all YouTube Live video practical series of experimental Pharmacology click:
https://youtube.com/playlist?list=PLBVbJ9HCa1Ba6WSJjeBaK0HMF79hdad3g
For More Such Learning You Can Subscribe to
My YouTube Channel:
https://www.youtube.com/channel/UC5o-WkzmDJaF7udyAP2jtgw/featured?sub_confirmation=1
Facebook Page: https://www.facebook.com/asacademylearningforever
Website Blog: https://itasacademy.blogspot.com/
Antiallergic activity by mast cell stabilization assayHimikaRathi
This document describes procedures for evaluating the antiallergic and mast cell stabilizing activity of drugs. It involves using guinea pigs to test if drugs can prevent bronchoconstriction induced by histamine aerosol exposure. It also involves collecting mast cells from rat peritoneal fluid and observing if drugs can prevent degranulation when exposed to egg albumin. The procedures provide a way to test if drugs can stabilize mast cell membranes and prevent the release of inflammatory mediators associated with allergic responses.
This document discusses QSAR (quantitative structure-activity relationship), which is a mathematical model that relates biological activity to physicochemical properties of molecules. QSAR can be used to predict activity of new compounds. Key parameters used in QSAR include hydrophobicity (measured by partition coefficient), electronic effects (Hammett constant), and steric effects (Taft's steric factor). These parameters influence drug absorption, distribution, and interactions with receptors. QSAR models take the form of biological activity = function(parameters) to develop relationships between activity and molecular properties.
This document presents information on parasympathomimetics, which are drugs that mimic the effects of parasympathetic nervous system stimulation. It discusses how parasympathomimetics can directly activate cholinergic receptors through agonists like acetylcholine, muscarine, and pilocarpine. It also describes how anticholinesterase drugs inhibit the acetylcholinesterase enzyme, increasing the availability of acetylcholine at cholinergic synapses. Specific parasympathomimetic drugs discussed include bethanechol, carbachol, pilocarpine, and echothiophate. The document provides details on the mechanisms of action and therapeutic uses of these cholinergic drugs.
SAR versus QSAR, History and development of QSAR, Types of physicochemical
parameters, experimental and theoretical approaches for the determination of
physicochemical parameters such as Partition coefficient, Hammet’s substituent
constant and Taft’s steric constant. Hansch analysis, Free Wilson analysis, 3D-QSAR
approaches like COMFA and COMSIA.
Herbs, Herbal Drugs
Present Scope of Herbal Drug Industry
Scope of Herbal Drug Medicine and Industry
Indian Herbal Industry
International Scope of Herbal Medicines
World Wide Herbal Trade
Overview on plant based industries and research institutions in India
List of few herbal drug industries in India
List of few herbal research institution/ centres in India
General Introduction to Herbal Industry
Herbal drugs industry: Present scope and future prospects.
A brief account of plant based industries and institutions involved in work on medicinal and
aromatic plants in India.
Combinatorial chemistry allows for the rapid synthesis of large libraries of compounds. It works by synthesizing many structures in parallel rather than one at a time. There are two main approaches: solid phase synthesis which attaches compounds to resin beads to isolate products, and solution phase which synthesizes in solvent. The libraries can be screened to identify active compounds more efficiently than traditional methods. This technique has increased the success of drug discovery by allowing testing of more structures at once.
Drug-plasma protein binding plays a key role in drug pharmacokinetics and pharmacodynamics. Proteins, particularly albumin and alpha-1-acid glycoprotein, bind drugs reversibly through mechanisms like hydrogen bonding, hydrophobic interactions, and van der Waals forces. Only the unbound fraction of a drug is active, as protein-bound drug is inert and cannot cross membranes or exert effects. Several factors influence protein binding, including drug properties, protein concentrations, and disease states. The degree of protein binding impacts drug absorption, distribution, metabolism, and elimination.
The document discusses prodrugs, which are pharmacologically inactive derivatives of active drugs designed to improve drug properties like solubility, absorption, and site-specific delivery. It covers basic prodrug concepts and classifications like carrier-linked prodrugs and bioprecursors. Approaches for prodrug design include using carriers, linkers, and multi-drug systems. Applications of prodrugs include improving patient acceptability by modifying taste, odor or irritation, enhancing solubility and dissolution for better absorption, and enabling site-specific or sustained drug delivery. The document provides examples of prodrug linkages and enzymes involved in their hydrolysis.
This document discusses protein drug binding, including the mechanisms, classes, and factors that influence it. It begins by introducing protein drug binding and defining it as the formation of a complex between a drug and a protein. This binding can be reversible or irreversible. There are several mechanisms of binding including hydrogen bonds, hydrophobic bonds, ionic bonds, and Van der Waals forces. Protein drug binding is important as it influences the absorption, distribution, metabolism, and excretion of drugs. The extent of protein binding is affected by characteristics of the drug and protein as well as disease states and interactions between drugs. In summary, this document provides an overview of the topic of protein drug binding, including the key concepts and significance.
This document discusses the mechanisms of drug absorption in the gastrointestinal (GI) tract. There are three main categories of mechanisms: 1) transcellular/intracellular transport, which involves permeation across cell membranes; 2) paracellular/intercellular transport through spaces between cells; and 3) vesicular or corpuscular transport via endocytosis. Transcellular transport includes both passive processes like diffusion and active processes requiring energy. Paracellular transport occurs through tight junctions or temporary openings between cells. Vesicular transport involves engulfing materials in membrane vesicles.
Respiratory stimulants are drugs that stimulate respiration and can restore consciousness in coma or fainting. They work by directly activating the respiratory center or through reflex action. At low doses, they stimulate respiration, but the margin of safety is narrow, and high doses can cause convulsions. Their role in therapeutics is limited, as they may be used in conditions like overdose with sedatives until mechanical ventilation, suffocation from drowning, or respiratory depression after anesthesia or in premature infants. Respiratory stimulants are classified as those acting directly on the respiratory center, those acting through reflex action, or those with mixed mechanisms of action. Doxapram, for example, promotes excitation of central neurons controlling
This document discusses physiological salt solutions used to maintain tissues outside the body. Standard salt solutions are poor substitutes for blood due to issues like coagulation, oxygenation, and nutrient availability for bacteria. Various solutions are described for different tissue types, with key ingredients like sodium, potassium, calcium, magnesium, and buffers. Methods for delivering the solutions to tissues include perfusion, tissue baths, and superfusion. Precautions are discussed for preparing, using, and storing the solutions.
Herbal Drug Technology (B.Pharm. 6th Semester)
Definition of herbs, herbal medicine, herbal medicinal product, herbal drug preparation
Source of herbs, Selection, identification and authentication of herbal materials,
Processing of herbal raw material
This document discusses renal and non-renal routes of drug excretion. It describes the key organs and processes involved in excretion, including the nephron in renal excretion and factors that determine if a drug is excreted renally or non-renally. Non-renal excretion includes biliary excretion through the liver and bile ducts. Clearance, excretion ratio, and other pharmacokinetic concepts relating to measurement of excretion are also covered.
This document provides a synopsis for a Master's thesis project titled "Formulation and Evaluation of Fast Dissolving Films of Lisinopril". The project aims to develop fast dissolving films of the hypertension drug Lisinopril to improve patient compliance. Literature on fast dissolving drug delivery systems and films has been reviewed. The planned work involves preparing Lisinopril films using natural and synthetic polymers through various techniques and evaluating the films for properties like drug content, dissolution, and pharmacodynamics. If successful, the fast dissolving Lisinopril films could provide quick action and ease of administration benefits for hypertension patients.
This document provides an overview of bioassay procedures. It defines bioassay as the comparative assessment of the potency of a test compound to a standard compound using a living biological system. The basic bioassay procedure involves preparing tissues, attaching them to an organ bath, constructing dose-response curves for standard and test compounds, and calculating the potency of the test compound based on its curve's position relative to the standard. Sources of error include biological variation between tissues and methodological errors in experimental design or implementation.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Expt 8 Effect of drugs on ciliary motility of frog oesophagusMirza Anwar Baig
This document outlines a study to examine the effect of various drugs on gastrointestinal motility using frogs. The study will use physostigmine and atropine solutions applied to the buccal cavity of frogs to measure the time taken for food particles to move from the lower jaw to the esophagus, compared to a saline control. The goal is to determine if physostigmine enhances while atropine reduces gastrointestinal motility by stimulating or blocking acetylcholine, respectively. The procedure describes preparing the frog, taking baseline measurements, then applying the drug solutions and remeasuring motility times to observe any effects.
Ideas for pharmacy students on final year project : Possible Research FieldsTareq ✅
This document provides ideas for pharmacy students' final year projects. It outlines four main research fields: pharmacy practice, pharmaceutics, chemistry, and pharmacognosy. Some potential project topics include surveys of new drugs, formulation of different dosage forms, synthesis of new medicinal drugs, and bioassays of plant extracts for biological activities. The document was prepared by Tareq Tareq, a B.Pharm student at the International Islamic University Chittagong in Bangladesh.
This document discusses patenting aspects of traditional knowledge and natural products, using the cases of turmeric and neem. It defines traditional knowledge and intellectual property rights, explaining that patents provide legal protection for inventions. It then describes the patenting process and requirements, such as an invention being novel, non-obvious, and useful. The document outlines what can and cannot be patented for natural products. It provides examples of patented formulations, new uses of herbal constituents, and isolation or modification of natural compounds. The case studies detail how India challenged and had a turmeric wound-healing patent revoked for lack of novelty, as well as a neem patent dispute.
Expt 11 Effect of drugs on locomotor activity using actophotometerMirza Anwar Baig
This document describes an experiment to evaluate the effects of drugs on locomotor activity using an actophotometer. Rats or mice are injected with either a saline control, the antipsychotic drug chlorpromazine at 3 mg/kg, or caffeine at 3 mg/kg. Their movement is then measured in the actophotometer before and after drug administration. Chlorpromazine is expected to reduce locomotor activity as a CNS depressant, while caffeine may increase it as a CNS stimulant. The results are presented as locomotor activity scores showing that chlorpromazine decreased activity and caffeine increased it, demonstrating their respective CNS effects.
University Institute of Pharmaceutical Sciences is a flag bearer of excellence in Pharmaceutical education and research in the country. Here is another initiative to make study material available to everyone worldwide. Based on the new PCI guidelines and syllabus here we have a presentation dealing with pharmacokinetics : concept of linear and non-linear compartment models.
Thank you for reading.
Hope it was of help to you.
UIPS,PU team
This document outlines World Health Organization (WHO) and International Council for Harmonization (ICH) guidelines for evaluating herbal drugs. It discusses evaluating the quality, safety, efficacy and intended use of herbal medicines according to WHO guidelines. This includes assessing the botanical identity and constituents of plant materials, manufacturing processes, stability testing, safety, efficacy based on literature and traditional use, and providing product information for consumers. ICH guidelines on quality and safety are also used to assess drug substances. The overall aim is to help regulatory authorities and manufacturers properly evaluate herbal drugs.
Expt 10 Effects of skeletal muscle relaxants using rota-rod apparatusMirza Anwar Baig
This document presents a study on the effects of the skeletal muscle relaxant diazepam using a rota-rod apparatus. Mice were given injections of diazepam and their ability to remain on a rotating rod was measured and compared to untreated mice. Treatment with diazepam significantly decreased the time mice could spend on the rotating rod, indicating that diazepam has muscle relaxing properties. The study aims to evaluate diazepam's muscle relaxation effects using a non-invasive method that observes the loss of muscle grip in animals.
The IUPHAR/BPS Guide to PHARAMCOLOGY in 2018: new features and updatesGuide to PHARMACOLOGY
2018 update poster for the IUPHAR/BPS Guide to PHARMACOLOGY. Giving details of new features and updates. To be presented at Pharmacology Futures, Edinburgh, May 2018; ELIXIR-All Hands, Berlin, June 2018 and World Congress of Pharmacology, Kyoto, Japan, July 2018
Poster presented at the Elixir All-Hands Meeting in Lisbon, June 2019. Gives a broad summary of Guide to Pharmacology activities in the last year. Emphasising new tools and our extension into malaria pharmacology.
Combinatorial chemistry allows for the rapid synthesis of large libraries of compounds. It works by synthesizing many structures in parallel rather than one at a time. There are two main approaches: solid phase synthesis which attaches compounds to resin beads to isolate products, and solution phase which synthesizes in solvent. The libraries can be screened to identify active compounds more efficiently than traditional methods. This technique has increased the success of drug discovery by allowing testing of more structures at once.
Drug-plasma protein binding plays a key role in drug pharmacokinetics and pharmacodynamics. Proteins, particularly albumin and alpha-1-acid glycoprotein, bind drugs reversibly through mechanisms like hydrogen bonding, hydrophobic interactions, and van der Waals forces. Only the unbound fraction of a drug is active, as protein-bound drug is inert and cannot cross membranes or exert effects. Several factors influence protein binding, including drug properties, protein concentrations, and disease states. The degree of protein binding impacts drug absorption, distribution, metabolism, and elimination.
The document discusses prodrugs, which are pharmacologically inactive derivatives of active drugs designed to improve drug properties like solubility, absorption, and site-specific delivery. It covers basic prodrug concepts and classifications like carrier-linked prodrugs and bioprecursors. Approaches for prodrug design include using carriers, linkers, and multi-drug systems. Applications of prodrugs include improving patient acceptability by modifying taste, odor or irritation, enhancing solubility and dissolution for better absorption, and enabling site-specific or sustained drug delivery. The document provides examples of prodrug linkages and enzymes involved in their hydrolysis.
This document discusses protein drug binding, including the mechanisms, classes, and factors that influence it. It begins by introducing protein drug binding and defining it as the formation of a complex between a drug and a protein. This binding can be reversible or irreversible. There are several mechanisms of binding including hydrogen bonds, hydrophobic bonds, ionic bonds, and Van der Waals forces. Protein drug binding is important as it influences the absorption, distribution, metabolism, and excretion of drugs. The extent of protein binding is affected by characteristics of the drug and protein as well as disease states and interactions between drugs. In summary, this document provides an overview of the topic of protein drug binding, including the key concepts and significance.
This document discusses the mechanisms of drug absorption in the gastrointestinal (GI) tract. There are three main categories of mechanisms: 1) transcellular/intracellular transport, which involves permeation across cell membranes; 2) paracellular/intercellular transport through spaces between cells; and 3) vesicular or corpuscular transport via endocytosis. Transcellular transport includes both passive processes like diffusion and active processes requiring energy. Paracellular transport occurs through tight junctions or temporary openings between cells. Vesicular transport involves engulfing materials in membrane vesicles.
Respiratory stimulants are drugs that stimulate respiration and can restore consciousness in coma or fainting. They work by directly activating the respiratory center or through reflex action. At low doses, they stimulate respiration, but the margin of safety is narrow, and high doses can cause convulsions. Their role in therapeutics is limited, as they may be used in conditions like overdose with sedatives until mechanical ventilation, suffocation from drowning, or respiratory depression after anesthesia or in premature infants. Respiratory stimulants are classified as those acting directly on the respiratory center, those acting through reflex action, or those with mixed mechanisms of action. Doxapram, for example, promotes excitation of central neurons controlling
This document discusses physiological salt solutions used to maintain tissues outside the body. Standard salt solutions are poor substitutes for blood due to issues like coagulation, oxygenation, and nutrient availability for bacteria. Various solutions are described for different tissue types, with key ingredients like sodium, potassium, calcium, magnesium, and buffers. Methods for delivering the solutions to tissues include perfusion, tissue baths, and superfusion. Precautions are discussed for preparing, using, and storing the solutions.
Herbal Drug Technology (B.Pharm. 6th Semester)
Definition of herbs, herbal medicine, herbal medicinal product, herbal drug preparation
Source of herbs, Selection, identification and authentication of herbal materials,
Processing of herbal raw material
This document discusses renal and non-renal routes of drug excretion. It describes the key organs and processes involved in excretion, including the nephron in renal excretion and factors that determine if a drug is excreted renally or non-renally. Non-renal excretion includes biliary excretion through the liver and bile ducts. Clearance, excretion ratio, and other pharmacokinetic concepts relating to measurement of excretion are also covered.
This document provides a synopsis for a Master's thesis project titled "Formulation and Evaluation of Fast Dissolving Films of Lisinopril". The project aims to develop fast dissolving films of the hypertension drug Lisinopril to improve patient compliance. Literature on fast dissolving drug delivery systems and films has been reviewed. The planned work involves preparing Lisinopril films using natural and synthetic polymers through various techniques and evaluating the films for properties like drug content, dissolution, and pharmacodynamics. If successful, the fast dissolving Lisinopril films could provide quick action and ease of administration benefits for hypertension patients.
This document provides an overview of bioassay procedures. It defines bioassay as the comparative assessment of the potency of a test compound to a standard compound using a living biological system. The basic bioassay procedure involves preparing tissues, attaching them to an organ bath, constructing dose-response curves for standard and test compounds, and calculating the potency of the test compound based on its curve's position relative to the standard. Sources of error include biological variation between tissues and methodological errors in experimental design or implementation.
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Expt 8 Effect of drugs on ciliary motility of frog oesophagusMirza Anwar Baig
This document outlines a study to examine the effect of various drugs on gastrointestinal motility using frogs. The study will use physostigmine and atropine solutions applied to the buccal cavity of frogs to measure the time taken for food particles to move from the lower jaw to the esophagus, compared to a saline control. The goal is to determine if physostigmine enhances while atropine reduces gastrointestinal motility by stimulating or blocking acetylcholine, respectively. The procedure describes preparing the frog, taking baseline measurements, then applying the drug solutions and remeasuring motility times to observe any effects.
Ideas for pharmacy students on final year project : Possible Research FieldsTareq ✅
This document provides ideas for pharmacy students' final year projects. It outlines four main research fields: pharmacy practice, pharmaceutics, chemistry, and pharmacognosy. Some potential project topics include surveys of new drugs, formulation of different dosage forms, synthesis of new medicinal drugs, and bioassays of plant extracts for biological activities. The document was prepared by Tareq Tareq, a B.Pharm student at the International Islamic University Chittagong in Bangladesh.
This document discusses patenting aspects of traditional knowledge and natural products, using the cases of turmeric and neem. It defines traditional knowledge and intellectual property rights, explaining that patents provide legal protection for inventions. It then describes the patenting process and requirements, such as an invention being novel, non-obvious, and useful. The document outlines what can and cannot be patented for natural products. It provides examples of patented formulations, new uses of herbal constituents, and isolation or modification of natural compounds. The case studies detail how India challenged and had a turmeric wound-healing patent revoked for lack of novelty, as well as a neem patent dispute.
Expt 11 Effect of drugs on locomotor activity using actophotometerMirza Anwar Baig
This document describes an experiment to evaluate the effects of drugs on locomotor activity using an actophotometer. Rats or mice are injected with either a saline control, the antipsychotic drug chlorpromazine at 3 mg/kg, or caffeine at 3 mg/kg. Their movement is then measured in the actophotometer before and after drug administration. Chlorpromazine is expected to reduce locomotor activity as a CNS depressant, while caffeine may increase it as a CNS stimulant. The results are presented as locomotor activity scores showing that chlorpromazine decreased activity and caffeine increased it, demonstrating their respective CNS effects.
University Institute of Pharmaceutical Sciences is a flag bearer of excellence in Pharmaceutical education and research in the country. Here is another initiative to make study material available to everyone worldwide. Based on the new PCI guidelines and syllabus here we have a presentation dealing with pharmacokinetics : concept of linear and non-linear compartment models.
Thank you for reading.
Hope it was of help to you.
UIPS,PU team
This document outlines World Health Organization (WHO) and International Council for Harmonization (ICH) guidelines for evaluating herbal drugs. It discusses evaluating the quality, safety, efficacy and intended use of herbal medicines according to WHO guidelines. This includes assessing the botanical identity and constituents of plant materials, manufacturing processes, stability testing, safety, efficacy based on literature and traditional use, and providing product information for consumers. ICH guidelines on quality and safety are also used to assess drug substances. The overall aim is to help regulatory authorities and manufacturers properly evaluate herbal drugs.
Expt 10 Effects of skeletal muscle relaxants using rota-rod apparatusMirza Anwar Baig
This document presents a study on the effects of the skeletal muscle relaxant diazepam using a rota-rod apparatus. Mice were given injections of diazepam and their ability to remain on a rotating rod was measured and compared to untreated mice. Treatment with diazepam significantly decreased the time mice could spend on the rotating rod, indicating that diazepam has muscle relaxing properties. The study aims to evaluate diazepam's muscle relaxation effects using a non-invasive method that observes the loss of muscle grip in animals.
The IUPHAR/BPS Guide to PHARAMCOLOGY in 2018: new features and updatesGuide to PHARMACOLOGY
2018 update poster for the IUPHAR/BPS Guide to PHARMACOLOGY. Giving details of new features and updates. To be presented at Pharmacology Futures, Edinburgh, May 2018; ELIXIR-All Hands, Berlin, June 2018 and World Congress of Pharmacology, Kyoto, Japan, July 2018
Poster presented at the Elixir All-Hands Meeting in Lisbon, June 2019. Gives a broad summary of Guide to Pharmacology activities in the last year. Emphasising new tools and our extension into malaria pharmacology.
This document provides an overview of the International Union of Basic and Clinical Pharmacology Guide to Pharmacology (GtoPdb) database. It describes the database contents including over 1,700 drug targets and 9,400 ligands. The database is curated by 500 experts and provides target and ligand information for researchers. Specialized versions of the database have also been created for immunopharmacology and malaria research.
The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb) is an open, expert-driven database that contains information on over 1,700 pharmacological targets and the substances that act on them. The database provides overviews and detailed information on targets that is manually curated from literature and reviewed by experts. It aims to cover human drug targets and potential future therapeutic targets. New features of the database include search tools to find targets and ligands, information on diseases associated with targets and ligands, organization of ligand families, and comparison of ligand activity across species. The database content is available to download in various formats and its interoperability has been increased through developing an RDF version and submitting data to other sources
The document summarizes recent updates to the IUPHAR/BPS Guide to PHARMACOLOGY database. It describes new features including expanded target coverage with over 1,700 drug targets and 1,100 related proteins. A new Pharmacology Search Tool allows users to upload protein lists and find associated ligands. The database also now connects immunopharmacology by associating targets with immune processes, cell types, and diseases. Additionally, the guide describes collaborations to include antimalarial compound data and develop an IUPHAR/MMV Guide to Malaria Pharmacology.
The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb) is an expert-driven, open database of pharmacological targets and the substances that act on them. It contains information on over 1,800 drug targets and 1,100 related proteins. The database is curated by 500 experts and provides detailed pharmacological data as well as overviews of key properties and ligands. Specialized extensions of GtoPdb include guides to immunopharmacology and malaria pharmacology that connect their fields to drug discovery. The database is continuously updated with new targets, ligands, features and access methods.
Poster on GtoImmuPdb presented at European Congress of Immunology (Amsterdam, Sep 2018). Overview of the main data types and features included in this extension to the IUPHAR/BPS Guide to PHARMACOLOGY
Guide to PHARMACOLOGY: a web-Based Compendium for Research and EducationChris Southan
This document summarizes a presentation about the IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb) database. The following key points are made:
- GtoPdb is an online resource containing information on over 8,000 ligands and their interactions with around 1,500 human protein targets. It has been used widely by researchers and educators since 2009.
- The database contains detailed information on drug targets like GPCRs, ion channels, and enzymes. It also provides data on ligands, drugs, interactions between ligands and targets, and related clinical information.
- Users can browse targets and ligands or search the database. Detailed target pages contain pharmacology data, mechanisms, and links
Assessing GtoPdb ligand content in PubChemChris Southan
The document discusses the content of ligands from the IUPHAR/BPS Guide to PHARMACOLOGY database (GtoPdb) that is contained within PubChem. It finds that GtoPdb ligands have extensive overlap with several other sources within PubChem, including patents, DrugBank, vendor structures, bioassays, and ChEMBL. This overlap allows users to find additional information on GtoPdb ligands from these complementary sources within PubChem.
Poster titled "The imperative of small, high quality data for underpinning big data: the IUPHAR/BPS Guide to PHARMACOLOGY". Presented by Dr. Christopher Southan, at the British Society of Pharmacology, Institute for Translational Medicine & Therapeutics (ITMAT) Meeting, Edinburgh, March 2017, ‘Big Data & the Development of New Medicines’.
Analysing curated protein targets: Partitioning the drugged and the druggable Chris Southan
The document summarizes the Guide to Pharmacology (GtoPdb) database, which curates ligand-protein interaction data from the literature. The database captures interactions between 1460 proteins and 7733 ligands from over 5000 references. It facilitates analysis of drug targets and comparison of druggable targets with compounds tested in vivo. The document then analyzes the genome ontology classifications of targets in the database compared to all human proteins, showing enrichment of receptors, enzymes and transporters in druggable targets. It also provides breakdowns of target characteristics like pathway membership and transmembrane domains. Finally, it uses Venn diagrams to compare targets of approved drugs with high vs. low affinity ligands, showing high-affinity drugs are biased toward receptors.
Drug-to-protein mappings in the Guide to PHARMACOLOGY: Utility as a target va...Guide to PHARMACOLOGY
The Guide to Pharmacology database (GtoPdb) provides expertly curated information on drug-protein interactions and targets of approved and investigational drugs. It currently includes data on interactions between over 1400 protein targets and 7700 ligands derived from over 5000 literature references. The database covers major target classes and provides a useful resource for target validation and drug discovery. Future plans include regular updates with new target and drug data as well as potential specialty sub-portals within the database.
This document summarizes and compares different sources of data on the druggable proteome, including the IUPHAR/BPS Guide to Pharmacology (GtoPdb), ChEMBL, DrugBank, BindingDB, and Swiss-Prot. It finds that these sources have some unique and overlapping protein targets. Only 3.4% of human proteins are covered by all four main sources. The document discusses expanding the druggable proteome through new modalities and probes, as well as challenges such as validation costs and reproducibility issues.
The GtoImmuPdb Portal aims to provide a unique access point for immunological data within the Guide to Pharmacology (GtoPdb) database. It will contain expert-curated immunological information on protein targets and ligands tagged as immunologically relevant. The portal will assist in identifying potential drug targets and experimental molecules for testing, and will link targets and ligands to immunological processes, cell types, and related diseases. A beta version of GtoImmuPdb is scheduled for release in Spring 2017.
IUPHAR/BPS Guide to PHARMACOLOGY in 2017: new features and updatesGuide to PHARMACOLOGY
This document summarizes updates to the IUPHAR/BPS Guide to PHARMACOLOGY database. It provides expert curated data on human drug targets and ligands. Recent additions include new target families, ligands, and links to immunopharmacology data. New features include download options, search tools, and organization of ligand families. The database is maintained by an international team and network of scientists and provides a resource for pharmacology education and research.
IUPHAR Guide to IMMUNOPHARMACOLOGY poster. Presented at the BSI Congress 2017, Brighton, UK (6th December 2017) and at Pharmacology 2017, London, UK (13th December 2017.
Enzymes as drug targets: curated pharmacological information in the 'Guide to...Guide to PHARMACOLOGY
Presented at the British Pharmacological Society Focused meeting in April 2015, this poster summarises the current coverage of our curation of enzyme drug targets and supplements our previous poster covering this target class
IUPHAR/BPS Guide to Pharmacology: concise mapping of chemistry, data, and tar...Chris Southan
The document summarizes the IUPHAR/BPS Guide to Pharmacology (GtoPdb) database, which maps relationships between chemistry, data, and protein targets. It has evolved from earlier databases to now include over 1500 human protein targets linked to ligand data. Challenges include resolving relationships across different target hierarchies and filling data gaps. Future plans include expanding the database and linking it to immunopharmacology data through a new Guide to Immunopharmacology portal.
Presentation by Dr. Elena Faccenda on the IUPHAR/BPS Guide to Immunopharmacology at the 39° Congresso Nazionale della Società Italiana di Farmacologia in Florence, Nov 2019
This document discusses the IUPHAR/BPS Guide to Pharmacology database and related resources. It provides open access information on pharmacological targets and the substances that act on them. It includes over 1,700 human drug targets, 9,700 ligands including 1,300 approved drugs. Related databases include the Guide to Immunopharmacology and Guide to Malaria Pharmacology. The databases are regularly updated and include links to other resources to enable interoperability.
1) Researchers have created a new online resource called the IUPHAR/MMV Guide to Malaria Pharmacology (GtoMPdb) to curate information on antimalarial compounds and their molecular targets in Plasmodium.
2) The database currently contains 25 Plasmodium molecular targets and 57 antimalarial ligands that were manually curated from scientific literature.
3) A new customized online portal provides open access to the antimalarial data and allows browsing by parasite lifecycle stage, target species, and other features to help malaria research.
The document provides an overview and progress report on database activities from April 2018 - March 2019. Key points include:
- Publications in peer-reviewed journals on the database and new immunopharmacology guide.
- Engagement through conferences, social media, and interactions with users seeking to improve the database.
- Ongoing development of the database interface and content, including expansion to new therapeutic areas.
- Statistics on usage, file downloads, and web service calls that show increasing interaction over time.
Dr. Simon D. Harding of the University of Edinburgh created a knowledge-base that connects immunology and pharmacology. The knowledge-base links immunological targets and ligands to cell types and diseases. It is part of the IUPHAR/BPS Guide to Pharmacology, an open database of drug targets and ligands including approved drugs. A new search tool allows searching of pharmacological information. Dr. Harding also aims to curate data on antimalarial compounds and their molecular targets in Plasmodium through the IUPHAR/MMV Guide to Malaria Pharmacology.
The document provides an overview and status report of the Core Guide to PHARMACOLOGY (GtoPdb) database. It discusses recent publications from the team, compliance with new GDPR privacy regulations, website access statistics showing increased usage, new website features, and priorities for further development such as expanding disease and content coverage.
The document provides a status report on the Guide to Immunopharmacology database (GtoImmuPdb). It discusses developments including the addition of disease data, graphical browsing of cell type data, and process data. The database is in beta version 3 and undergoing user testing. Over 500 targets and 1,000 ligands have been curated from the literature. On the curation side, efforts are focused on expanding the literature collection and annotating new targets and ligands. The database is preparing for its official launch in October 2018.
Updated poster following beta v3 release. In preparation for Pharmacology Futures, Edinburgh Immunology Symposium and Word Congress of Pharmacology (Kyoto)
These slides will be presented at the Pharmacology 2017 meeting in London during the following session:
Abstract Number: OB073
Abstract Title: Capturing new BIA 10-2474 molecular data in the IUPHAR/BPS Guide to PHARMACOLOGY
Date: Wednesday, December 13, 2017, 11:30 AM
Oral Session: Oral Communications: Mixed Tracks
This comprehensive slide deck is provided for use by those who are teaching and presenting on the IUPHAR/BPS Guide to PHARMACOLOGY. Includes:
- Overview of NC-IUPHAR
- Background to GtoPdb
- Screenshots of the website and search tools
- Recent content expansions
- Other features and initiatives including the Guide to IMMUNOPHARMACOLOGY
This slide set updates the previous set from 2014/15 available at https://www.slideshare.net/GuidetoPHARM/iupharbps-guide-to-pharmacology-generic-slideset
Navigating links between structures and papers:
PubMed-to-PubChem connectivity between the IUPHAR/BPS Guide to PHARMACOLOGY and British Journal of Pharmacology
A poster presented at Pharmacology 2017, London, December 2017
A general poster about the IUPHAR/BPS Guide to PHARMACOLOGY, updated for 2017. This works well used as a handout or pinned on departmental noticeboards.
This document describes updates to the Guide to PHARMACOLOGY (GtoPdb) database in 2017, including new features such as:
1) Organization of drug targets into families and subclasses for easier browsing, and organization of ligands into related families and groups.
2) Ability to visualize ligand binding affinities across species through activity graphs.
3) SynPHARM database for finding ligand binding sequences that can be engineered into synthetic proteins.
4) Expanded content with over 1,700 drug targets, 9,000 ligands, and options to search or download data in various formats.
A Wellcome Trust-funded project to extend the Guide to PHARMACOLOGY (www.guidetopharmacology.org) to include data on key immunological data types and associate these to drugs and drug targets. Presented at the ELIXIR-UK All-Hand Meeting, Edinburgh, Nov 2017.
(First slide is recording of webinar). IUPHAR Web Resources, Simplifying Complexity for Medicine and Education. WDS Webinar#11 held on 28th February 2017.
IUPHAR (International Union of Basic and Clinical Pharmacology) has developed and is developing a series of web-based services for the Pharmacological Sciences, for education, and for drug discovery. These services enable the simplification and dissemination of highly complex datasets, via expert committees linked to ontologically-correct databases (e.g., the drug and receptor sites expressed by the human genome). This has also allowed IUPHAR—in connection with the main national pharmacological societies, particularly the British Pharmacological Society—to raise funds for curators and meetings. This simple model is open-ended and is being expanded to, for example, immunological targets and experimental protocols, and to educational projects.
Speakers: Michael Spedding, Adam Pawson, Steve Alexander, Joanna Sharman, Simon Harding, Jamie Davies, John Szarek and Lynn LeCount
Flash poster presentation slide of IUPHAR Guide to PHARMACOLOGY. As presented by Dr. Simon Harding at BPS Pharmacology 2016 @BritPharmSoc @GuidetoPHARM
This presentation offers a general idea of the structure of seed, seed production, management of seeds and its allied technologies. It also offers the concept of gene erosion and the practices used to control it. Nursery and gardening have been widely explored along with their importance in the related domain.
Mechanics:- Simple and Compound PendulumPravinHudge1
a compound pendulum is a physical system with a more complex structure than a simple pendulum, incorporating its mass distribution and dimensions into its oscillatory motion around a fixed axis. Understanding its dynamics involves principles of rotational mechanics and the interplay between gravitational potential energy and kinetic energy. Compound pendulums are used in various scientific and engineering applications, such as seismology for measuring earthquakes, in clocks to maintain accurate timekeeping, and in mechanical systems to study oscillatory motion dynamics.
SDSS1335+0728: The awakening of a ∼ 106M⊙ black hole⋆Sérgio Sacani
Context. The early-type galaxy SDSS J133519.91+072807.4 (hereafter SDSS1335+0728), which had exhibited no prior optical variations during the preceding two decades, began showing significant nuclear variability in the Zwicky Transient Facility (ZTF) alert stream from December 2019 (as ZTF19acnskyy). This variability behaviour, coupled with the host-galaxy properties, suggests that SDSS1335+0728 hosts a ∼ 106M⊙ black hole (BH) that is currently in the process of ‘turning on’. Aims. We present a multi-wavelength photometric analysis and spectroscopic follow-up performed with the aim of better understanding the origin of the nuclear variations detected in SDSS1335+0728. Methods. We used archival photometry (from WISE, 2MASS, SDSS, GALEX, eROSITA) and spectroscopic data (from SDSS and LAMOST) to study the state of SDSS1335+0728 prior to December 2019, and new observations from Swift, SOAR/Goodman, VLT/X-shooter, and Keck/LRIS taken after its turn-on to characterise its current state. We analysed the variability of SDSS1335+0728 in the X-ray/UV/optical/mid-infrared range, modelled its spectral energy distribution prior to and after December 2019, and studied the evolution of its UV/optical spectra. Results. From our multi-wavelength photometric analysis, we find that: (a) since 2021, the UV flux (from Swift/UVOT observations) is four times brighter than the flux reported by GALEX in 2004; (b) since June 2022, the mid-infrared flux has risen more than two times, and the W1−W2 WISE colour has become redder; and (c) since February 2024, the source has begun showing X-ray emission. From our spectroscopic follow-up, we see that (i) the narrow emission line ratios are now consistent with a more energetic ionising continuum; (ii) broad emission lines are not detected; and (iii) the [OIII] line increased its flux ∼ 3.6 years after the first ZTF alert, which implies a relatively compact narrow-line-emitting region. Conclusions. We conclude that the variations observed in SDSS1335+0728 could be either explained by a ∼ 106M⊙ AGN that is just turning on or by an exotic tidal disruption event (TDE). If the former is true, SDSS1335+0728 is one of the strongest cases of an AGNobserved in the process of activating. If the latter were found to be the case, it would correspond to the longest and faintest TDE ever observed (or another class of still unknown nuclear transient). Future observations of SDSS1335+0728 are crucial to further understand its behaviour. Key words. galaxies: active– accretion, accretion discs– galaxies: individual: SDSS J133519.91+072807.4
SAP Unveils Generative AI Innovations at Annual Sapphire ConferenceCGB SOLUTIONS
At its annual SAP Sapphire conference, SAP introduced groundbreaking generative AI advancements and strategic partnerships, underscoring its commitment to revolutionizing business operations in the AI era. By integrating Business AI throughout its enterprise cloud portfolio, which supports the world's most critical processes, SAP is fostering a new wave of business insight and creativity.
إتصل على هذا الرقم اذا اردت الحصول على "حبوب الاجهاض الامارات" توصيلنا مجاني رقم الواتساب 00971547952044:
00971547952044. حبوب الإجهاض في دبي | أبوظبي | الشارقة | السطوة | سعر سايتوتك Cytotec يتميز دواء Cytotec (سايتوتك) بفعاليته في إجهاض الحمل. يمكن الحصول على حبوب الاجهاض الامارات بسهولة من خلال خدمات التوصيل السريع والدفع عند الاستلام. تُستخدم حبوب سايتوتك بشكل شائع لإنهاء الحمل غير المرغوب فيه. حبوب الاجهاض الامارات هي الخيار الأمثل لمن يبحث عن طريقة آمنة وفعالة للإجهاض المنزلي.
تتوفر حبوب الاجهاض الامارات بأسعار تنافسية، ويمكنك الحصول على خصم كبير عند الشراء الآن. حبوب الاجهاض الامارات معروفة بقدرتها الفعالة على إنهاء الحمل في الشهر الأول أو الثاني. إذا كنت تبحث عن حبوب لتنزيل الحمل في الشهر الثاني أو الأول، فإن حبوب الاجهاض الامارات هي الخيار المثالي.
دواء سايتوتك يحتوي على المادة الفعالة ميزوبروستول، التي تُستخدم لإجهاض الحمل والتخلص من النزيف ما بعد الولادة. يمكنك الآن الحصول على حبوب سايتوتك للبيع في دبي وأبوظبي والشارقة من خلال الاتصال برقم 00971547952044. نسعى لتقديم أفضل الخدمات في مجال حبوب الاجهاض الامارات، مع توفير حبوب سايتوتك الأصلية بأفضل الأسعار.
إذا كنت في دبي، أبوظبي، الشارقة أو العين، يمكنك الحصول على حبوب الاجهاض الامارات بسهولة وأمان. نحن نضمن لك وصول الحبوب الأصلية بسرية تامة مع خيار الدفع عند الاستلام. حبوب الاجهاض الامارات هي الحل الفعال لإنهاء الحمل غير المرغوب فيه بطريقة آمنة.
تبحث العديد من النساء في الإمارات العربية المتحدة عن حبوب الاجهاض الامارات كبديل للعمليات الجراحية التي تتطلب وقتاً طويلاً وتكلفة عالية. بفضل حبوب الاجهاض الامارات، يمكنك الآن إنهاء الحمل بسلام وأمان في منزلك. نحن نوفر حبوب الاجهاض الامارات الأصلية من إنتاج شركة فايزر، مما يضمن لك الحصول على منتج فعال وآمن.
إذا كنت تبحث عن حبوب الاجهاض الامارات في العين، دبي، أو أبوظبي، يمكنك التواصل معنا عبر الواتس آب أو الاتصال على رقم 00971547952044 للحصول على التفاصيل حول كيفية الشراء والتوصيل. حبوب الاجهاض الامارات متوفرة بأسعار تنافسية، مع تقديم خصومات كبيرة عند الشراء بالجملة.
حبوب الاجهاض الامارات هي الخيار الأمثل لمن تبحث عن وسيلة آمنة وسريعة لإنهاء الحمل غير المرغوب فيه. تواصل معنا اليوم للحصول على حبوب الاجهاض الامارات الأصلية وتجنب أي مشاكل أو مضاعفات صحية.
في النهاية، لا تقلق بشأن الحبوب المقلدة أو الخطرة، فنحن نوفر لك حبوب الاجهاض الامارات الأصلية بأفضل الأسعار وخدمة التوصيل السريع والآمن. اتصل بنا الآن على 00971547952044 لتأكيد طلبك والحصول على حبوب الاجهاض الامارات التي تحتاجها. نحن هنا لمساعدتك وتقديم الدعم اللازم لضمان حصولك على الحل المناسب لمشكلتك.
TOPIC OF DISCUSSION: CENTRIFUGATION SLIDESHARE.pptxshubhijain836
Centrifugation is a powerful technique used in laboratories to separate components of a heterogeneous mixture based on their density. This process utilizes centrifugal force to rapidly spin samples, causing denser particles to migrate outward more quickly than lighter ones. As a result, distinct layers form within the sample tube, allowing for easy isolation and purification of target substances.
Evaluation and Identification of J'BaFofi the Giant Spider of Congo and Moke...MrSproy
ABSTRACT
The J'BaFofi, or "Giant Spider," is a mainly legendary arachnid by reportedly inhabiting the dense rain forests of
the Congo. As despite numerous anecdotal accounts and cultural references, the scientific validation remains more elusive.
My study aims to proper evaluate the existence of the J'BaFofi through the analysis of historical reports,indigenous
testimonies and modern exploration efforts.
Microbial interaction
Microorganisms interacts with each other and can be physically associated with another organisms in a variety of ways.
One organism can be located on the surface of another organism as an ectobiont or located within another organism as endobiont.
Microbial interaction may be positive such as mutualism, proto-cooperation, commensalism or may be negative such as parasitism, predation or competition
Types of microbial interaction
Positive interaction: mutualism, proto-cooperation, commensalism
Negative interaction: Ammensalism (antagonism), parasitism, predation, competition
I. Mutualism:
It is defined as the relationship in which each organism in interaction gets benefits from association. It is an obligatory relationship in which mutualist and host are metabolically dependent on each other.
Mutualistic relationship is very specific where one member of association cannot be replaced by another species.
Mutualism require close physical contact between interacting organisms.
Relationship of mutualism allows organisms to exist in habitat that could not occupied by either species alone.
Mutualistic relationship between organisms allows them to act as a single organism.
Examples of mutualism:
i. Lichens:
Lichens are excellent example of mutualism.
They are the association of specific fungi and certain genus of algae. In lichen, fungal partner is called mycobiont and algal partner is called
II. Syntrophism:
It is an association in which the growth of one organism either depends on or improved by the substrate provided by another organism.
In syntrophism both organism in association gets benefits.
Compound A
Utilized by population 1
Compound B
Utilized by population 2
Compound C
utilized by both Population 1+2
Products
In this theoretical example of syntrophism, population 1 is able to utilize and metabolize compound A, forming compound B but cannot metabolize beyond compound B without co-operation of population 2. Population 2is unable to utilize compound A but it can metabolize compound B forming compound C. Then both population 1 and 2 are able to carry out metabolic reaction which leads to formation of end product that neither population could produce alone.
Examples of syntrophism:
i. Methanogenic ecosystem in sludge digester
Methane produced by methanogenic bacteria depends upon interspecies hydrogen transfer by other fermentative bacteria.
Anaerobic fermentative bacteria generate CO2 and H2 utilizing carbohydrates which is then utilized by methanogenic bacteria (Methanobacter) to produce methane.
ii. Lactobacillus arobinosus and Enterococcus faecalis:
In the minimal media, Lactobacillus arobinosus and Enterococcus faecalis are able to grow together but not alone.
The synergistic relationship between E. faecalis and L. arobinosus occurs in which E. faecalis require folic acid
MICROBIAL INTERACTION PPT/ MICROBIAL INTERACTION AND THEIR TYPES // PLANT MIC...
Poster GtoPdb Pharmacology 2017
1. 3. Searching for targets and ligands
2. Current database content
8. References
1 Centre for Integrative Physiology, University of Edinburgh, Edinburgh, UK. 2 School of Life Sciences, University of Nottingham Medical School, Nottingham, UK. 3 Experimental
Medicine and Immunotherapeutics, University of Cambridge, Cambridge. 4 Spedding Research Solutions SAS, Paris, France. * The International Union of Basic and Clinical
Pharmacology Committee on Receptor Nomenclature and Drug Classification.
www.guidetopharmacology.org enquiries@guidetopharmacology.org @GuidetoPHARM
The IUPHAR/BPS Guide to PHARMACOLOGY
in 2017: new features and updates
Supported by:
We especially thank all contributors, collaborators and NC-IUPHAR members
1. Introduction
The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb) is an open, expert-driven
database of pharmacological targets and the substances that act on them [1]. It is a
joint initiative between the British Pharmacological Society (BPS) and the International
Union of Basic and Clinical Pharmacology (IUPHAR), which aims to cover the human
targets of licensed drugs and other likely targets of future therapeutics.
The information is presented at two levels:
1. Overviews of the key properties, selective ligands and further reading for a wide
range of human biological targets, which form the basis for the Concise Guide to
PHARMACOLOGY (CGTP) [2].
2. Detailed pharmacological, functional and clinical information for a subset of
important targets.
All data are manually curated from the primary literature and reviewed by an
international network of >500 experts in 96 subcommittees of the IUPHAR Committee
on Receptor Nomenclature and Drug Classification (NC-IUPHAR).
~1,700 established or potential data-supported drug targets
~1,100 additional related proteins
• G protein-coupled receptors (GPCRs), including Orphan GPCRs & Adhesion GPCRs
• Voltage-gated ion channels (VGICs)
• Ligand-gated ion channels (LGICs)
• Other ion channels
• Nuclear hormone receptors (NHRs)
• Enzymes, including kinases & proteases
• Catalytic receptors
• Transporters
~9,000 ligands
• Approved drugs
• Experimental compounds & labelled ligands
• Hormones, neurotransmitters, metabolites
• Endogenous and synthetic peptides
• Antibodies
• Natural products
• Inorganic chemicals
Various search tools are available to find targets and ligands by keyword (Fig. 2),
identifier, reference, chemical structure (Fig. 3), or protein sequence (Fig. 4).
Figure 1. Examples of various kinase database tables
1. Harding SD, et al. (2018) The IUPHAR/BPS Guide to PHARMACOLOGY in 2018: Updates and expansion to encompass
the new Guide to IMMUNOPHARMACOLOGY. Nucl. Acids Res. 46 (Database Issue). doi: 10.1093/nar/gkx1121.
2. Alexander SPH, et al. (2017) The Concise Guide to PHARMACOLOGY 2017/18. Br J Pharmacol. 174 (Suppl 1): S1-
S446.
3. Bento AP, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. 42 (Database Issue): D1083-
D1090.
4. Rose PW, et al. (2017) The RCSB protein data bank: integrative view of protein, gene and 3D structural information. Nucl
Acids Res, 45 (Database Issue), D271-D281.Figure 4. BLAST sequence search for targets
GtoPdb is an ELIXIR UK node resource
Figure 2. Target name search
with autocomplete function
Figure 3. Chemical structure search
4. Navigating target and ligand families
Targets are organised by class, which can be browsed as a tree with families and
subfamilies (Fig. 5). Ligands have also recently been organised into related families and
groups (Fig. 6). Each family/group page lists summary information for the ligands, with
links to more detailed pages (Fig. 7).
Figure 5. Target families
Joanna L. Sharman1, Elena Faccenda1, Simon D. Harding1, Adam J. Pawson1, Christopher Southan1, Stephen P.H.
Alexander2, Anthony P. Davenport3, Michael Spedding4, Jamie A. Davies1 and NC-IUPHAR*
6. SynPHARM database of ligand binding sequences
SynPHARM is a tool for finding ligand binding sequences which can be engineered into
synthetic proteins to confer drugability. It combines pharmacological parameters from
GtoPdb with ligand binding data from the RCSB Protein Data Bank [4] (Fig. 9).
It is freely available at http://synpharm.guidetopharmacology.org.
Figure 9. (A/B) The location of a ligand binding sequence is shown in green on a protein
structure. (C) A residue distance matrix indicating ‘globularity’ of the sequence. The
dotted line represents the binding sequence – the greener the area is the more
compact the sequence.
A B C
5. Comparing ligand affinity across species
Ligand activity graphs provide a quick way to visualise affinity at different targets and
across species. Box plots (Fig. 8A) summarise standardised activity data from GtoPdb
and ChEMBL [3]. Individual data points, assay details and references are provided in an
accompanying table (Fig. 8B).
Figure 8. Chart and table showing palosuran activity at human and rat UT receptors
Figure 1. Examples of data types for NHRs
Figure 6. Ligand families
Figure 7. A ligand family summary page
A B
7. Downloading data
Data are available to download in various formats:
• Lists of targets, ligands and interactions in CSV format
• REST web services for computational access to data in JSON format
• SQL database dump files
• Interaction data are now available in RDF format for semantic integration