Targeting a kinase? Find out how BMG LABTECH microplate readers measure interaction with kinases, kinase activities and kinase inhibitors in high throughput.
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.
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.
Identiﬁcation of false positives in a HTRF screen for small molecule inhibitors of PD-1/PD-L1Michael Speake , Stuart McElroy , , BioAscent Discovery Limited, Newhouse, UK, 06/2021
Binding kinetics: high throughput assay for kinase inhibitorsKrumm A (1) , Georgi V (2) , Schiele F (2) , Fernández-Montalván A (2), (1) BMG LABTECH GmbH , (2) Bayer AG, Drug Discovery, Pharmaceuticals, Berlin, Germany, 06/2020
Dual Channel Kinetic assays for detecting ligand bias at GPCRsPaul Tewson (1) , Scott Martinka (1) , Kevin M. Harlen (1) , Thom Hughes (1) , Anne Marie Quinn (1) , Sam R.J. Hoare (2) , Carl Peters (3), (1) Montana Molecular, Bozeman, MT , (2) Pharmechanics, Owego, NY , (3) BMG LABTECH Inc., NC, USA, 11/2019
Analyze binding kinetics with HTRFNicolas Pierre , Thomas Roux, Cisbio Bioassays, Codolet, France, 05/2019
NanoBRET™ assay quantitatively evaluates VEGF binding to the VEGFR2 in real-time in living cellsKilpatrick LE (1) , Friedman-Ohana R (2) , Alcobia DC (1) , Riching K (2) , Peach CJ (1) , Wheal AJ (1) , Briddon SJ (1) , Robers MB (2) , Zimmerman K (2) , Machleidt T (2) , Wood KV (2) , Woolard J (1) , Hill SJ (1), (1) Division of Physiology, Pharmacology and Neuroscience, University of Nottingham, UK , (2) Promega Corporation, Madison, WI, USA, 01/2018
Monoclonal antibody drugs – a history of success and a bright future!
High-throughput screening (HTS)
Lab Automation – Pipetting many thousands of samples by hand is awful
Identification of harmine and β-carboline analogs from a high-throughput screen of an approved drug collection; profiling as differential inhibitors of DYRK1A and monoamine oxidase A and for in vitro and in vivo anti-cancer studiesRead article
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
Pharmacological targeting of the novel β-catenin chromatin-associated kinase p38α in colorectal cancer stem cell tumorspheres and organoidsRead article
Cell death & disease
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in MiceRead article
Journal of medicinal chemistry
Tunable Methacrylamides for Covalent Ligand Directed Release ChemistryRead article
Journal of the American Chemical Society
The ellagic acid metabolites urolithin A and B differentially affect growth, adhesion, motility, and invasion of endometriotic cells in vitroRead article
Human reproduction (Oxford, England)