Drug Screening

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.

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.

    • A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes

      Mai, QN;Shenoy, P;Quach, T;Retamal, JS;Gondin, AB;Yeatman, HR;Aurelio, L;Conner, JW;Poole, DP;Canals, M;Nowell, CJ;Graham, B;Davis, TP;Briddon, SJ;Hill, SJ;Porter, CJH;Bunnett, NW;Halls, ML;Veldhuis, NA;[2021]

      The Journal of biological chemistry

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    • Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70

      Li, Y;Lin, W;Wright, WC;Chai, SC;Wu, J;Chen, T;[2021]

      Journal of medicinal chemistry

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    • A Fbxo48 inhibitor prevents pAMPKα degradation and ameliorates insulin resistance

      Liu, Y;Jurczak, MJ;Lear, TB;Lin, B;Larsen, MB;Kennerdell, JR;Chen, Y;Huckestein, BR;Nguyen, MK;Tuncer, F;Jiang, Y;Monga, SP;O'Donnell, CP;Finkel, T;Chen, BB;Mallampalli, RK;[2021]

      Nature chemical biology

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    • Investigation of Receptor Heteromers Using NanoBRET Ligand Binding

      Johnstone, EKM;See, HB;Abhayawardana, RS;Song, A;Rosengren, KJ;Hill, SJ;Pfleger, KDG;[2021]

      International journal of molecular sciences

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    • Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2

      Berger, BT;Amaral, M;Kokh, DB;Nunes-Alves, A;Musil, D;Heinrich, T;Schröder, M;Neil, R;Wang, J;Navratilova, I;Bomke, J;Elkins, JM;Müller, S;Frech, M;Wade, RC;Knapp, S;[2021]

      Cell chemical biology

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