Kinases
Targeting a kinase? Find out how BMG LABTECH microplate readers measure interaction with kinases, kinase activities and kinase inhibitors in high throughput.
Measuring thousands of wells in minutes, as needed for compound screens, requires extremely fast and sensitive instrumentation – the perfect task for BMG LABTECH plate readers.
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 multi-mode 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.
Competition assay using Fluorescence Polarization to determine the Residence Times for Calcitonin and AMYR agonist, AM833
Inform yourself here about the benefits of an alternative to (TR-)FRET-/BRET-based competition assays using FP for the determination of kon and koff of ligand/receptor interaction.
The ‘Advanced Assay Stability’ system facilitates a stable detection environment for temperature-sensitive assays
Difficulties comparing your results due to temperature variations? Read here how the cooling function of the PHERAstar FSX with AAS enables stable temperature and circumvents these problems.
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.
PROTACs: proteolysis-targeting chimeras
PROTACs are small, readily designed molecules that target unwanted proteins to the cell’s ubiquitin-proteasome system for degradation. Find out how microplate readers can advance PROTAC research.
Drug solubility: why testing early matters in drug discovery
Measuring light scattering is an accurate and expedient way to determine drug solubility. Find out how the NEPHELOstar® Plus can be used for early drug solubility screening at high throughput.
Mitochondrial toxicity: measurement and applications
Mitochondrial toxicity can have devastating effects on the cell and life. Find out how microplate readers can be used to assess mitochondrial health and how this impacts disease and drug discovery.
Binding kinetics
The investigation of binding kinetics is crucial for drug research. Find out, how binding kinetics work and which approaches can be used to study them on microplate readers.
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.
Protocol to utilize fresh uncultured human lung tumor cells for personalized functional diagnostics
Talwelkar, SS;Lähdeniemi, IAK;Mäyränpää, MI;Hemmes, A;Linnavirta, N;Räsänen, J;Knuuttila, A;Wennerberg, K;Verschuren, EW; [2022]
STAR protocols 3(4) 101720
Design, Synthesis, Antiviral Evaluation, and Molecular Dynamics Simulation Studies of New Spirocyclic Thiopyrimidinones as Anti HCoV-229E
Ragab, SS;Sweed, AMK;Elrashedy, AA;Allayeh, AK; [2022]
Chemistry & biodiversity e202200632
High throughput analysis of vacuolar acidification
Zhang, C;Balutowski, A;Feng, Y;Calderin, JD;Fratti, RA; [2022]
Analytical 60988327696 658 114927
Discovery of Benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain
Cipriano, A;Milite, C;Feoli, A;Viviano, M;Pepe, G;Campiglia, P;Sarno, G;Picaud, S;Imaide, S;Makukhin, N;Filippakopoulos, P;Ciulli, A;Castellano, S;Sbardella, G; [2022]
ChemMedChem e202200343
Design and in vitro/in vivo Evaluation of Polyelectrolyte Complex Nanoparticles Filled in Enteric-Coated Capsules for Oral Delivery of Insulin
Arpaç, B;Devrim Gökberk, B;Küçüktürkmen, B;Özakca Gündüz, I;Palabıyık, İM;Bozkır, A; [2022]
Journal of pharmaceutical sciences
Gefitinib Inhibits Rifampicin-Induced CYP3A4 Gene Expression in Human Hepatocytes
Abbott, KL;Salamat, JM;Flannery, PC;Chaudhury, CS;Chandran, A;Vishveshwara, S;Mani, S;Huang, J;Tiwari, AK;Pondugula, SR; [2022]
ACS omega 7(38) 34034-34044
Targeting the type 1 cholecystokinin receptor to screen for novel obesity treatments
Development of functional, binding and multiplex assays targeting the type 1 cholecystokinin receptor to screen for potential new compounds against obesity.
Binding affinity determination on microplate readers
Binding affinity is an important parameter in drug discovery. Find out, how microplate readers can be used for binding affinity determination and the advantages they offer.
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.
Taking a wholistic approach to automation
Mathew Keegan talks about the seamless integration of BMG LABTECH plate readers into Automata´s system
From assay development to compound screening
Joao used a CLARIOstar Plus and a PHERAstar FSX, for assay development and compound screening against a viral exonuclease.
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.
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