Kinases
Targeting a kinase? Find out how BMG LABTECH microplate readers measure interaction with kinases, kinase activities and kinase inhibitors in high throughput.
HTS & drug discovery
Measuring thousands of wells in minutes, as it is needed for compound screens, requires extremely fast and sensitive instrumentation. Read why BMG LABTECH plate readers are heavily used in screening laboratories.
An essential part of the early phase of drug discovery is screening libraries of compounds in order to detect potential ‘hits’ which interact with a therapeutic target. Common targets include membrane proteins such as GPCRs as well as kinases and PROTACS. Compounds acting on a therapeutic target have to be identified out of libraries of thousands to millions of compounds, making automation of the process using microplate readers essential.
Screens are mainly conducted in 384 and 1536 well plates to minimize reaction volumes per sample. Speed and sensitivity are key requirements for screeners. A 1536 well microplate needs to be measured in seconds, maximally a few minutes. Furthermore, the fast measurement of 10 µl or even lower volume samples needs to be very precise and stable to clearly identify hits from a vast number of compounds. In addition, the reader needs to be reliable, as errors occurring during a screen result in repetitions, loss of time, reagents and consequently money.
BMG LATBECH’s microplate readers have market leading performance ensuring hits can be reliably detected at low volumes and at the fastest speeds. This not only enables the highest throughput but also allows rapid cycle times in kinetic assays required for studying binding kinetics and on/off rates.
The PHERAstar FSX masters all these requirements in all detection modes, making it popular in screening facilities. For screening assay development and testing, the CLARIOstar Plus is the perfect addition to develop and characterize an assay before transitioning to high throughput.
Take a look at the links below to find out more about our instruments and how they have been used by drug screeners.
Receptors
GPCRs are the top drug targets. Numerous assays study ligand binding, receptor signaling, or binding kinetics in high throughput. Measure them on a single reader.
Resources
Search our resources section for information about specific applications, literature citations, videos, blog articles and many other publications. Many of the resources provided are associated with current and previous instrument models and versions.
Viral Cytopathic effects measured in a drug discovery screen
Are you looking for a label-free method to study potential antiviral drugs? This AppNote presents a fast and cheap way to study viral cytopathic effects with cell viability/toxicity assays.
Identification of false positives in a HTRF® screen for small molecule inhibitors of PD-1/PD-L1
Are you tired of false positive hits affecting your results? In this application note you will find two options for identifying false positive compounds via HTRF measurement.
Antiviral assay based on expression of fluorescent proteins by the viruses
Are you looking for an easy way to screen for antivirals in 384-well format? This application is ideally suited to investigate virus uptake and replication in living cells.
High-throughput ELISA ready to analyse in 90-minutes: 384-well SimpleStep ELISA® with the PHERAstar® FSX
Did you know, that the 90 min SimpleStep ELISA®s by abcam also work in 384-well format? Read here why our dedicated high-throughput reader PHERAstar® FSX is the perfect match for HTS.
Studying the molecular mechanism of viral replication in real time using the CLARIOstar Plus with ACU
Looking for methods to study the molecular mechanisms of viral replication? In this AppNote a fluorescence-based approach for real-time measurement of viral gene expression is presented.
Binding kinetics: high throughput assay for kinase inhibitors
Studying binding kinetics helps to reduce clinical failure of potential drugs. Read here, how TR-FRET can be used to determine association and dissociation rates of unlabelled compounds.
NanoBRET
NanoBRET is used to analyse binding events, signaling pathways and receptor trafficking in live cells and has significantly expanded the range and applications of BRET assays.
Binding Assays - More Than One Way to Achieve your Goals
Overwhelmed with the abundance of assay options? This blog compares the various advantages and disadvantages of different approaches available for binding assays.
How to determine binding affinity with a microplate reader?
The determination and optimisation of binding affinity are of great importance for the development of new drugs and treatment options. Read more here.
Transcreener assays
Read here how you can perform Transcreener® assays to e.g. quantify AMP on the powerful and sensitive microplate readers from BMG LABTECH.
Monoclonal antibody drugs – a history of success and a bright future!
The use of monoclonal antibody drugs for therapeutic outcomes remains a topic of high interest throughout the research community. Read more on their history and promises here.
High-throughput screening (HTS)
What is high-throughput screening (HTS) and how can it be used? Find out, why BMG LABTECH microplate readers are perfect tools for HTS approaches.
HTS Identification of Activators and Inhibitors of Endoplasmic Reticulum (ER) Stress and the Unfolded Protein Response (UPR)
Ghafouri, M;Gauss, CB;Fribley, AM; [2022]
Methods in molecular biology (Clifton, N.J.) 2378 317-327
Aurora Kinase A Is Involved in Controlling the Localization of Aquaporin-2 in Renal Principal Cells
Baltzer, S;Bulatov, T;Schmied, C;Krämer, A;Berger, BT;Oder, A;Walker-Gray, R;Kuschke, C;Zühlke, K;Eichhorst, J;Lehmann, M;Knapp, S;Weston, J;von Kries, JP;Süssmuth, RD;Klussmann, E; [2022]
International journal of molecular sciences 23(2)
Neuropeptide B/W receptor 1 peptidomimetic agonists: Structure-activity relationships and plasma stability
Nguyen, T;Decker, AM;Snyder, RW;Tonetti, EC;Gamage, TF;Zhang, Y; [2022]
European journal of medicinal chemistry 231 114149
Evaluation of SARS-CoV-2 entry, inflammation and new therapeutics in human lung tissue cells
Grau-Expósito, J;Perea, D;Suppi, M;Massana, N;Vergara, A;Soler, MJ;Trinite, B;Blanco, J;García-Pérez, J;Alcamí, J;Serrano-Mollar, A;Rosado, J;Falcó, V;Genescà, M;Buzon, MJ; [2022]
PLoS pathogens 18(1) e1010171
Bacterial Indole as a Multifunctional Regulator of Klebsiella oxytoca Complex Enterotoxicity
Ledala, N;Malik, M;Rezaul, K;Paveglio, S;Provatas, A;Kiel, A;Caimano, M;Zhou, Y;Lindgren, J;Krasulova, K;Illes, P;Dvořák, Z;Kortagere, S;Kienesberger, S;Cosic, A;Pöltl, L;Zechner, EL;Ghosh, S;Mani, S;Radolf, JD;Matson, AP; [2022]
mBio e0375221
Discovery and Characterization of Novel Antagonists of the Proinflammatory Orphan Receptor GPR84
Jenkins, L;Marsango, S;Mancini, S;Mahmud, ZA;Morrison, A;McElroy, SP;Bennett, KA;Barnes, M;Tobin, AB;Tikhonova, IG;Milligan, G; [2021]
ACS pharmacology & translational science 4(5) 1598-1613
Using the TRUPATH BRET platform to analyse GPCR biased agonism
TRUPATH is a BRET-based platform that enables to monitor discrete GPCR-G protein coupling and can facilitate the discovery of drugs biased towards desired G protein effectors.
Current microplate-based interaction assays for drug discovery
Protein-protein interaction is the key in physiological processes - and likewise many diseases. Learn here about possible approaches to study interactions in drug screening using NanoBRET and TR-FRET.
Kinetics in Drug Discovery
Martin Redhead, group leader at UCB, discusses the use and impact of kinetic binding methods across the drug discovery pipeline.
Miniaturising screening assays: a case study
Watch here, how the PHERAstar’s extraordinary sensitivity allows to detect TR-FRET assays with high reliability and reproducibility even in miniaturized sample volumes using 1536-well plates.
Cell-based and biochemical high-throughput screening in 1536-well plates
Learn more on successful miniaturization approaches and high-throughput screening attempts in 1536-well plates employing the CRISPR/Cas9 system to knock in Nano luciferase reporter genes.
A TR-FRET approach to measure the kinetics of ligand-receptor binding and its application of fragment screening
Leave radioactive assays behind: the PHERAstar provides temporal resolution to determine kon and koff rates by TR-FRET binding kinetics.
Simplifying laboratory automation
David Reed (Managing Director at Flexible Lab Solutions) talks about the seamless integration of the BMG LABTECH microplate reader PHERAstar FSX into this system.
High-throughput screening of cyclic peptide libraries for developing drugs to challenging targets
Prof. Heinis´ work focusses on the use of cyclic peptides as drugs. Here he discusses the benefits of this approach and in how the PHERAstar FSX supports his screening needs.
Searching for optimised drugs: combining AI with human expertise
Read in this interview how Martin Redhead from Exscientia searches for optimised drugs and combines AI with human expertise.
Streamlined and more efficient drug screening with the PHERAstar FSX
Zaida Gloria talks about why she chose the PHERAstar FSX and how this plate reader makes her job easier.
Improving hit discovery efficiency at Europe’s leading screening centre
Read in this interview with Steven van Helden,Chief Technology Officer at Pivot Park Screening Centre (PPSC), how you can improve your hit discovery efficiency.
Choosing the best microplate reader
Efficient microplate readers play an important role in effective hit molecule discovery. Mark Wigglesworth, of AstraZeneca, explains what he looks for in this technology.
PHERAstar FSX
Powerful and most sensitive HTS plate reader
CLARIOstar Plus
Most flexible Plate Reader for Assay Development
NEPHELOstar Plus
Microplate nephelometer for light-scattering and turbidity measurements