The DOI matches its Crossref record; 55 of the 55 references it cites were found in a registry or an index.
New assay technologies for high-throughput screening
Abstract
The use of high-throughput screening for early stage drug discovery imposes several constraints on the format of assays for therapeutic targets of interest. Homogeneous cell-free assays based on energy transfer, fluorescence polarization spectroscopy or fluorescence correlation spectroscopy provide the sensitivity, ease, speed and resistance to interference from test compounds needed to function in a high-throughput screening mode. Similarly, novel cell-based assays are now being adapted for high-throughput screening, providing for in situ analysis of a variety of biological targets. Finally, recent advances in assay miniaturization mark a transition to ultra high-throughput screening, ensuring that identification of lead compounds will not be the rate-limiting step in finding new drugs.
Overview
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
Citations
Cites
Fluorescent indicators for Ca2+based on green fluorescent proteins and calmodulin
Miyawaki, A., Llopis, J. L., Heim, R., McCaffery, J. M., Adams, J. A., Ikura, M., & Tsien, R. Y. (1997) · Nature · doi:10.1038/42264 · Cited by 3,250
Heim, R., & Tsien, R. Y. (1996) · Current Biology · doi:10.1016/s0960-9822(02)00450-5 · Cited by 1,490
Transcriptional Regulation by Extracellular signals: Mechanisms and Specificity
Hill, C. S., & Treisman, R. (1995) · Cell · doi:10.1016/0092-8674(95)90403-4 · Cited by 1,012
Sorting single molecules: application to diagnostics and evolutionary biotechnology.
Eigen, M., & Rigler, R. W. (1994) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.91.13.5740 · Cited by 961
Zlokarnik, G., Negulescu, P. A., Knapp, T. E., Mere, L., Burres, N. S., Feng, L., Whitney, M. A., Roemer, K., & Tsien, R. Y. (1998) · Science · doi:10.1126/science.279.5347.84 · Cited by 691
Lenormand, P., Sardet, C., Pagès, G., L’Allemain, G., Brunet, A., & Pouysségur, J. (1993) · The Journal of Cell Biology · doi:10.1083/jcb.122.5.1079 · Cited by 660
Chemokine receptors: Gateways to inflammation and infection
Premack, B. A., & Schall, T. J. (1996) · Nature Medicine · doi:10.1038/nm1196-1174 · Cited by 630
Complex formation between RAS and RAF and other protein kinases.
Aelst, L. V., Barr, M. M., Marcus, S., Polverino, A. J., & Wigler, M. H. (1993) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.90.13.6213 · Cited by 620
A β-Arrestin/Green Fluorescent Protein Biosensor for Detecting G Protein-coupled Receptor Activation
Barak, L. S., Ferguson, S. S. G., Zhang, J., & Caron, M. G. (1997) · Journal of Biological Chemistry · doi:10.1074/jbc.272.44.27497 · Cited by 428
Rare earth cryptates and homogeneous fluoroimmunoassays with human sera
Mathis, G. (1993) · Clinical Chemistry · doi:10.1093/clinchem/39.9.1953 · Cited by 393
Microchip Device for Performing Enzyme Assays
Hadd, A. G., Raymond, D. E., Halliwell, J., Jacobson, S. C., & Ramsey, J. M. (1997) · Analytical Chemistry · doi:10.1021/ac970192p · Cited by 383
Applications of the green fluorescent protein in cell biology and biotechnology
Misteli, T., & Spector, D. L. (1997) · Nature Biotechnology · doi:10.1038/nbt1097-961 · Cited by 357
Mathis, G. (1995) · Clinical Chemistry · doi:10.1093/clinchem/41.9.1391 · Cited by 339
González, F. M., Seth, A., Raden, D. L., Bowman, D., Fay, F., & Davis, R. J. (1993) · The Journal of Cell Biology · doi:10.1083/jcb.122.5.1089 · Cited by 320
Mammalian Glucocorticoid Receptor Derivatives Enhance Transcription in Yeast
Schena, M., & Yamamoto, K. R. (1988) · Science · doi:10.1126/science.3043665 · Cited by 309
Mitra, R. D., Silva, C. M., & Youvan, D. C. (1996) · Gene · doi:10.1016/0378-1119(95)00768-7 · Cited by 302
TNF-Induced Activation of NF-κB
Schütze, S., Wiegmann, K., Machleidt, T., & Krönke, M. (1995) · Immunobiology · doi:10.1016/s0171-2985(11)80543-7 · Cited by 251
King, K., Dohlman, H. G., Thorner, J. W., Caron, M. G., & Lefkowitz, R. J. (1990) · Science · doi:10.1126/science.2171146 · Cited by 228
A Bioluminescent Assay for Agonist Activity at Potentially Any G-Protein-Coupled Receptor
Stables, J., Green, A. R., Marshall, F. H., Fraser, N., KNIGHT, E. L., Sautel, M., Milligan, G., Lee, M., & Rees, S. (1997) · Analytical Biochemistry · doi:10.1006/abio.1997.2308 · Cited by 199
Kralli, A., Bohen, S. P., & Yamamoto, K. R. (1995) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.92.10.4701 · Cited by 160
Tumour necrosis factor α and interleukin 1 signalling: do MAPKK kinases connect it all?
Eder, J. (1997) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(97)01097-3 · Cited by 148
Scintillation proximity assay: a versatile high-throughput screening technology
Cook, N. D. (1996) · Drug Discovery Today · doi:10.1016/1359-6446(96)10026-x · Cited by 138
Functional Coupling of a Mammalian Somatostatin Receptor to the Yeast Pheromone Response Pathway
Price, L. A., Kajkowski, E. M., Hadcock, J. R., Ozenberger, B. A., & Pausch, M. H. (1995) · Molecular and Cellular Biology · doi:10.1128/mcb.15.11.6188 · Cited by 132
Anderson, M. T., Tjioe, I., Lorincz, M. C., Parks, D. R., Herzenberg, L. A., Nolan, G. P., & Herzenberg, L. A. (1996) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.93.16.8508 · Cited by 106
Murakami, A., Nakaura, M., Nakatsuji, Y., Nagahara, S., Tran-Cong, Q., & Makino, K. (1991) · Nucleic Acids Research · doi:10.1093/nar/19.15.4097 · Cited by 99
Udenfriend, S., Gerber, L., & Nelson, N. (1987) · Analytical Biochemistry · doi:10.1016/0003-2697(87)90479-9 · Cited by 94
A paradigm for drug discovery employing encoded combinatorial libraries.
Burbaum, J. J., Ohlmeyer, M. H. J., Reader, J. C., Henderson, I. M., Dillard, L. W., Li, G., Randle, T. L., SIGAL, N. H., Chelsky, D., & Baldwin, J. J. (1995) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.92.13.6027 · Cited by 90
A Fluorescence Polarization Based Src-SH2 Binding Assay
Lynch, B. A., Loiacono, K. A., Tiong, C. L., Adams, S. E., & MacNeil, I. A. (1997) · Analytical Biochemistry · doi:10.1006/abio.1997.2042 · Cited by 89
Chemiluminescence: sensitive detection technology for reporter gene assays
Bronstein, I., Martin, C., Fortin, J. J., Olesen, C. E. M., & Voyta, J. C. (1996) · Clinical Chemistry · doi:10.1093/clinchem/42.9.1542 · Cited by 81
Tumour necrosis factor α and interleukin 1 signalling: do MAPKK kinases connect it all?
Eder, J. (1997) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(97)90657-x · Cited by 78
A Homogeneous, Fluorescence Polarization Assay for Src-Family Tyrosine Kinases
Seethala, R., & Menzel, R. (1997) · Analytical Biochemistry · doi:10.1006/abio.1997.2365 · Cited by 73
A miniaturized arrayed assay format for detecting small molecule-protein interactions in cells
You, A., Jackman, R. J., Whitesides, G. M., & Schreiber, S. L. (1997) · Chemistry & Biology · doi:10.1016/s1074-5521(97)90305-7 · Cited by 71
Dual Luminescence-Based Reporter Gene Assay for Luciferase andβ-Galactosidase
Martin, C., Wight, P. A., Dobretsova, A., & Bronstein, I. (1996) · BioTechniques · doi:10.2144/96213pf01 · Cited by 66
Functional expression of a vertebrate inwardly rectifying K+ channel in yeast.
Tang, W., RUKNUDIN, A. M., Yang, W. P., Shaw, S. Y., Knickerbocker, A., & Kurtz, S. E. (1995) · Molecular Biology of the Cell · doi:10.1091/mbc.6.9.1231 · Cited by 66
Hall, B. L., Smit‐McBride, Z., & Privalsky, M. L. (1993) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.90.15.6929 · Cited by 64
A High-Throughput STAT Binding Assay Using Fluorescence Polarization
Wu, P., Brasseur, M., & Schindler, U. (1997) · Analytical Biochemistry · doi:10.1006/abio.1997.2158 · Cited by 62
Schullek, J. R., Butler, J. H., Ni, Z., Chen, D., & Yuan, Z. (1997) · Analytical Biochemistry · doi:10.1006/abio.1996.9958 · Cited by 61
Braunwalder, A. F., Yarwood, D. R., Sills, M. A., & Lipson, K. E. (1996) · Analytical Biochemistry · doi:10.1006/abio.1996.0269 · Cited by 59
Measurement of Specific Protease Activity Utilizing Fluorescence Polarization
Levine, L. M., Michener, M. L., Toth, M. V., & Holwerda, B. C. (1997) · Analytical Biochemistry · doi:10.1006/abio.1997.2047 · Cited by 59
Craig, D., Arriaga, E. A., Banks, P., Zhang, Y., Renborg, A., Palcic, M. M., & Dovic̀hi, N. J. (1995) · Analytical Biochemistry · doi:10.1006/abio.1995.1202 · Cited by 55
Schade, S. Z., Jolley, M. E., Sarauer, B. J., & Simonson, L. G. (1996) · Analytical Biochemistry · doi:10.1006/abio.1996.0475 · Cited by 53
Chemiluminescent reporter gene assays: sensitive detection of the GUS and SEAP gene products.
Bronstein, I., Fortin, J. J., Voyta, J. C., Juo, R. R., Edwards, B., Olesen, C. E. M., Lijam, N., & Kricka, L. J. (1994) · PubMed · Cited by 50
Sterrer, S., & Henco, K. (1997) · Journal of Receptors and Signal Transduction · doi:10.3109/10799899709036624 · Cited by 46
Functional interaction of ligands and receptors of the hematopoietic superfamily in yeast.
Ozenberger, B. A., & Young, K. H. (1995) · Molecular Endocrinology · doi:10.1210/mend.9.10.8544840 · Cited by 43
Single-reagent polarization fluoroimmunoassay for amphetamine in urine.
Colbert, D. L., Gallacher, G., & Mainwaring-Burton, R. W. (1985) · Clinical Chemistry · doi:10.1093/clinchem/31.7.1193 · Cited by 38
Wei, A.-P., & Herron, J. N. (1993) · Analytical Chemistry · doi:10.1021/ac00071a007 · Cited by 37
Selection of an Optimal Reporter Gene for Cell-Based High Throughput Screening Assays
Suto, C. M., & Ignar, D. M. (1997) · SLAS DISCOVERY · doi:10.1177/108705719700200103 · Cited by 32
Ozenberger, B. A. (1995) · Molecular Endocrinology · doi:10.1210/me.9.10.1321 · Cited by 25
Recombinant Microorganisms as Tools for High Throughput Screening for Nonantibiotic Compounds
Klein, R. D., & Geary, T. G. (1997) · SLAS DISCOVERY · doi:10.1177/108705719700200108 · Cited by 23
Single-reagent polarization fluoroimmunoassay of methamphetamine in urine.
Eremin, S. A., Gallacher, G., Lotey, H., Smith, D. S., & Landon, J. (1987) · Clinical Chemistry · doi:10.1093/clinchem/33.10.1903 · Cited by 22
Reporter Assays in the High Throughput Screening Laboratory: A Rapid and Robust First Look?
Dhundale, A., & Goddard, C. P. (1996) · SLAS DISCOVERY · doi:10.1177/108705719600100303 · Cited by 20
Gaarde, W. A., Hunter, T. R., Brady, H. A., Murray, B. W., & Goldman, M. E. (1997) · SLAS DISCOVERY · doi:10.1177/108705719700200406 · Cited by 16
Lerner, C. G., & Saiki, A. Y. (1996) · Analytical Biochemistry · doi:10.1006/abio.1996.0348 · Cited by 15
Fluorescence polarization immunoassay of estradiol.
Aucouturier, P., Jl, P., & Lubochinsky, B. (1983) · PubMed · Cited by 7
Rogers, M. V. (1997) · Drug Discovery Today · doi:10.1016/s1359-6446(97)01101-x · Cited by 6
Cited by
Sorted by citations
The evolving role of natural products in drug discovery
Koehn, F. E., & Carter, G. T. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1657 · Cited by 2,579
“Advances in genomics and molecular biology have now made it possible to obtain relatively large quantities of protein targets for high-throughput, cell-free assay systems for directly detecting the catalytic inhibition or target bindin”
BackgroundA decade of fragment-based drug design: strategic advances and lessons learned
Hajduk, P., & Greer, J. (2007) · Nature reviews. Drug discovery · doi:10.1038/nrd2220 · Cited by 1,004
“To improve the chances of finding agents that are active against these targets, technologies such as combinatorial chemistry and ultra-high-throughput screening (HTS) approaches have considerably expanded the numbers of compounds that can be evaluated for their biological activit”
BackgroundThe Methylation Effect in Medicinal Chemistry
Barreiro, E. J., Kümmerle, A. E., & Fraga, C. A. M. (2011) · Chemical Reviews · doi:10.1021/cr200060g · Cited by 1,032
Modulators of Protein–Protein Interactions
Milroy, L.-G., Grossmann, T. N., Hennig, S., Brunsveld, L., & Ottmann, C. (2014) · Chemical Reviews · doi:10.1021/cr400698c · Cited by 497
Peptide-based biopolymers in biomedicine and biotechnology
Chow, D., Nunalee, M. L., Lim, D. W., Simnick, A. J., & Chilkoti, A. (2008) · Materials Science and Engineering R Reports · doi:10.1016/j.mser.2008.04.004 · Cited by 333
Metadata
- Authors
- Silverman, L., Campbell, R., & Broach, J. R.
- Affiliations
- Princeton University (US)
- Corresponding author
- Broach, James R
- Venue
- Current Opinion in Chemical Biology
- Publisher
- Elsevier BV
- Published
- 1998-06
- Volume
- 2
- Issue
- 3
- Pages
- 397-403
- ISSN
- 1367-5931 (ISSN-L)
- OpenAlex
- W2092399057
- Cited by
- 151
- References
- 55
- Citations by year
- 2025: 2 · 2023: 2 · 2022: 2 · 2021: 5 · 2020: 2 · 2019: 2 · 2016: 3 · 2015: 2 · 2014: 3 · 2013: 4 · 2012: 3
- FWCI
- 0.95
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Opinion in Chemical Biology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Advanced Biosensing Techniques and Applications
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
- Keywords
- high-throughput screening, fluorescence correlation spectroscopy, cell-based assays, assay miniaturization, ultra-high-throughput screening, lead compound identification, early drug discovery
- MeSH terms
- Animals, Cell Line, Cell-Free System, Chemistry, Organic, Drug Evaluation, Preclinical, Energy Transfer, Mammals, Miniaturization, Spectrometry, Fluorescence, Transfection, Drug Design, Genes, Reporter
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review