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
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
Inkjet printing for pharmaceutics – A review of research and manufacturing
Daly, R., Harrington, T. S., Martin, G. D., & Hutchings, I. M. (2015) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2015.03.017 · Cited by 318
High-Throughput Screening in Drug Metabolism and Pharmacokinetic Support of Drug Discovery
White, R. E. (2000) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.40.1.133 · Cited by 307
Fluorescence Spectroscopic Profiling of Compound Libraries
Simeonov, A. M., Jadhav, A., Thomas, C. J., Wang, Y., Huang, R., Southall, N. T., Shinn, P., Smith, J. A., Austin, C. P., Auld, D. S., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm701301m · Cited by 264
Ultrasensitive investigations of biological systems by fluorescence correlation spectroscopy
Haustein, E., & Schwille, P. (2003) · Methods · doi:10.1016/s1046-2023(02)00306-7 · Cited by 250
NMR-based screening in drug discovery
Hajduk, P. J., Meadows, R. P., & Fesik, S. W. (1999) · Quarterly Reviews of Biophysics · doi:10.1017/s0033583500003528 · Cited by 229
Stockwell, B. R., Haggarty, S. J., & Schreiber, S. L. (1999) · Chemistry & Biology · doi:10.1016/s1074-5521(99)80004-0 · Cited by 203
“To date, most cell-based assays have used reporter genes as an indicator of cellular activity [55].”
MethodA Decade of Yeast Surface Display Technology: Where Are We Now?
Shusta, E. V., Pepper, L. R., Cho, Y. K., & Boder, E. T. (2008) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/138620708783744516 · Cited by 189
The BRET technology and its application to screening assays
Bacart, J., Corbel, C., Jockers, R., Bach, S., & Couturier, C. (2008) · Biotechnology Journal · doi:10.1002/biot.200700222 · Cited by 178
“Reporter gene assays have been used to monitor receptor activation [72–75].”
MethodSurugiu, I., Danielsson, B. R. G., Ye, L., Mosbach, K., & Haupt, K. (2001) · Analytical Chemistry · doi:10.1021/ac0011540 · Cited by 157
Miniaturized HTS technologies – uHTS
Woelcke, J., & Ullmann, D. (2001) · Drug Discovery Today · doi:10.1016/s1359-6446(01)01807-4 · Cited by 147
Flavonoids: A complementary approach to conventional therapy of COVID-19?
Solnier, J., & Fladerer-Grollitsch, J.-P. (2020) · Phytochemistry Reviews · doi:10.1007/s11101-020-09720-6 · Cited by 149
Optical Imaging Fiber-Based Single Live Cell Arrays: A High-Density Cell Assay Platform
Biran, I., & Walt, D. R. (2002) · Analytical Chemistry · doi:10.1021/ac020009e · Cited by 132
Brock, R. E., Vámosi, G., Vereb, G., & Jovin, T. M. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.18.10123 · Cited by 131
Starr, T. E., & Thompson, N. L. (2001) · Biophysical Journal · doi:10.1016/s0006-3495(01)76130-9 · Cited by 127
“This technique is also of considerable current interest to the pharmaceutical community in that it has significant potential as a method for high throughput screening of drug–target interactions (Sterrer and Henco, 1997; Auer et al., 1998; Fister et al., 1998; Silverman et al., 1998; Moore et al., 2000).”
BackgroundMethodInfluentialAutomating solid-phase extraction: current aspecs and future prospekts
Rossi, D. T., & Zhang, N. R. (2000) · Journal of Chromatography A · doi:10.1016/s0021-9673(99)00984-x · Cited by 126
Materials for Non-Viral Gene Delivery
Segura, T., & Shea, L. D. (2001) · Annual Review of Materials Research · doi:10.1146/annurev.matsci.31.1.25 · Cited by 120
Technological Advances in High-Throughput Screening
Liu, B., Li, S., & Hu, J. (2004) · American Journal of PharmacoGenomics · doi:10.2165/00129785-200404040-00006 · Cited by 120
High impact technologies for natural products screening
Koehn, F. E. (2007) · Birkhäuser Basel eBooks · doi:10.1007/978-3-7643-8117-2_5 · Cited by 113
Ansede, J. H., & Thakker, D. R. (2003) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.10545 · Cited by 109
Turek-Etienne, T. C., Small, E. C., Soh, S. C., Xin, T. A., Gaitonde, P. V., Barrabee, E. B., Hart, R. F., & Bryant, R. W. (2003) · SLAS DISCOVERY · doi:10.1177/1087057103252304 · Cited by 102
Complex phenotypic assays in high-throughput screening
Clemons, P. A. (2004) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2004.04.002 · Cited by 101
Pharmaceutical intervention in the JAK/STAT signaling pathway
Seidel, H. M., Lamb, P., & Rosen, J. (2000) · Oncogene · doi:10.1038/sj.onc.1203550 · Cited by 97
“In addition to SPA assays, ¯uorescence-based assays using FRET (Stryer, 1978) or ¯uorescence polarization (FP) have been the most common solution to this problem (Silverman et al., 1998; Sittampalam et al., 1997).”
MethodBiomedical and Biotechnological Applications of Elastin-Like Polypeptides
Simnick, A. J., Lim, D. W., Chow, D., & Chilkoti, A. (2007) · Journal of macromolecular science. Part C, Reviews in macromolecular chemistry and physics/Journal of macromolecular science. Reviews in macromolecular chemistry and physics · doi:10.1080/15583720601109594 · Cited by 91
Novel miniaturized systems in high-throughput screening
Battersby, B. J., & Trau, M. (2002) · Trends in biotechnology · doi:10.1016/s0167-7799(01)01898-4 · Cited by 89
Automated Pharmacophore Identification for Large Chemical Data Sets
Chen, X., Rusinko, Tropsha, A., & Young, S. S. (1999) · Journal of Chemical Information and Computer Sciences · doi:10.1021/ci990327n · Cited by 81
Screening of Small Molecule Interactor Library by Using In-Cell NMR Spectroscopy (SMILI-NMR)
Xie, J., Thapa, R., Reverdatto, S., Burz, D. S., & Shekhtman, A. G. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm9000743 · Cited by 79
“In this work we show that: (1) the formation of a biocomplex is required to generate a high resolution NMR spectrum to study interacting molecules; (2) small molecule binding alters the interaction surfaces involved in biocomplex formation; (3) we can rapidly screen a library of small molecules to select compounds tha…”
BackgroundApplication of High-throughput Screening Techniques to Drug Discovery
Cox, B. J., Merritt, A. T., Binnie, A., Donnelly, M. C., Mander, T. H., Denyer, J. C., Evans, B., Green, D. V. S., Lewis, J. A., Valler, M. J., et al. (2000) · Progress in medicinal chemistry · doi:10.1016/s0079-6468(08)70058-4 · Cited by 77
Predicting human safety: screening and computational approaches
Johnson, D. E., & Wolfgang, G. H. I. (2000) · Drug Discovery Today · doi:10.1016/s1359-6446(00)01559-2 · Cited by 77
Sakamoto, S., Kabe, Y., Hatakeyama, M., Yamaguchi, Y., & Handa, H. (2009) · The Chemical Record · doi:10.1002/tcr.20170 · Cited by 76
Chan, N. W. C., Lewis, D. F., Rosner, P. J., Kelly, M. A., & Schriemer, D. C. (2003) · Analytical Biochemistry · doi:10.1016/s0003-2697(03)00193-3 · Cited by 72
Intracellular detection assays for high-throughput screening
González, J. E., & Negulescu, P. A. (1998) · Current Opinion in Biotechnology · doi:10.1016/s0958-1669(98)80141-9 · Cited by 72
Xu, H., Jia, Z., Xü, K., Zhou, H., & Shen, M. (2014) · Organic Letters · doi:10.1021/ol503247t · Cited by 71
Evans, S. E., Harrington, T. S., Rodríguez-Rivero, M. C., Rognin, E., Tuladhar, T. R., & Daly, R. (2021) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2021.120443 · Cited by 72
Nakajima, Y., & Ohmiya, Y. (2010) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2010.506213 · Cited by 67
RNA Conformation and Folding Studied with Fluorescence Resonance Energy Transfer
Klostermeier, D., & Millar, D. P. (2001) · Methods · doi:10.1006/meth.2000.1135 · Cited by 66
Moy, F. J., Haraki, K., Mobilio, D., Walker, G., Powers, R., Tabei, K., Tong, H., & Siegel, M. M. (2001) · Analytical Chemistry · doi:10.1021/ac0006270 · Cited by 66
Design of Adenosine Kinase Inhibitors from the NMR-Based Screening of Fragments
Hajduk, P. J., Gomtsyan, A. R., DiDomenico, S., Cowart, M., Bayburt, E. K., Solomon, L. R., Severin, J. M., Smith, R. A., Walter, K. A., Holzman, T. F., et al. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm000373a · Cited by 64
Synthetic polymers for biopharmaceutical delivery
Magnusson, J. P., Saeed, A. O., Fernández‐Trillo, F., & Alexander, C. (2010) · Polymer Chemistry · doi:10.1039/c0py00210k · Cited by 62
Modern Drug Discovery Technologies: Opportunities and Challenges in Lead Discovery
Guido, R. V. C., Oliva, G., & Andricopulo, A. D. (2011) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/138620711797537067 · Cited by 57
“In the pharmaceutical industry, the integration of combinatorial chemistry and HTS has become one of the most important ways for the identification of novel hits and leads in the early stages of the drug discovery process [32].”
BackgroundFunctional cell-based uHTS in chemical genomic drug discovery
Croston, G. E. (2002) · Trends in biotechnology · doi:10.1016/s0167-7799(02)01906-6 · Cited by 57
Berthier, E., Warrick, J. W., Yu, H., & Beebe, D. J. (2008) · Lab on a Chip · doi:10.1039/b717423c · Cited by 53
Molecular Fluorescence, Phosphorescence, and Chemiluminescence Spectrometry
Oldham, P. B., McCarroll, M. E., McGown, L. B., & Warner, I. M. (2000) · Analytical Chemistry · doi:10.1021/a1000017p · Cited by 49
Genetic Information, Genomic Technologies, and the Future of Drug Discovery
Bumol, T. F. (2001) · JAMA · doi:10.1001/jama.285.5.551 · Cited by 46
“Various analytical technologies have been used to develop highly leads for potential targets.(29,30) The types of drug candidates screened are originally derived from synthetic organic chemistry, combinatorial chemistry, which reflects parallel synthesis on chemical templates; natural product chemistry; and use of che…”
MethodHigh-Throughput Screening for Drug Discovery
Saxena, S. K. (2021) · IntechOpen eBooks · doi:10.5772/intechopen.91075 · Cited by 46
Creation of GPCR-based chemical sensors by directed evolution in yeast
Ault, A. D., & Broach, J. R. (2005) · Protein Engineering Design and Selection · doi:10.1093/protein/gzi069 · Cited by 45
“Yeast strains that have been utilized for functional analysis of GPCRs and drug screening were constructed by taking advantage of similarities between the yeast mating response pathway and human signal transduction pathways (Silverman et al., 1998).”
MethodSelf-citationProteomics in the post-genome age
Dongré, A. R., Opiteck, G. J., Cosand, W. L., & Hefta, S. A. (2001) · Biopolymers · doi:10.1002/1097-0282(2001)60:3 · Cited by 35
Seeing is believing: the impact of structural genomics on antimicrobial drug discovery
Schmid, M. B. (2004) · Nature Reviews Microbiology · doi:10.1038/nrmicro978 · Cited by 42
“Novel methods for biochemical high-throughput screening (HTS) were developed to meet the desire for automated homogenous and non-radioactive assay”
MethodNatural Products in Drug Discovery: Impacts and Opportunities — An Assessment
Brahmachari, G. (2011) · WORLD SCIENTIFIC eBooks · doi:10.1142/9789814335386_0001 · Cited by 45
Yoshimatsu, K., Ye, L., Stenlund, P., & Chronakis, I. S. (2008) · Chemical Communications · doi:10.1039/b719586a · Cited by 38
Saiz, C., Castillo, V., Fontán, P., Bonilla, M., Salinas, G., Rodríguez-Haralambides, A., & Mahler, G. (2013) · Molecular Diversity · doi:10.1007/s11030-013-9485-3 · Cited by 38
Rational Development of Caged-Biotin Protein-Labeling Agents and Some Applications in Live Cells
Terai, T., Maki, E., Sugiyama, S., Takahashi, Y., Matsumura, H., Mori, Y., & Nagano, T. (2011) · Chemistry & Biology · doi:10.1016/j.chembiol.2011.09.007 · Cited by 36
A general electrochemical method for label-free screening of protein–small molecule interactions
Cash, K. J., Ricci, F., & Plaxco, K. W. (2009) · Chemical Communications · doi:10.1039/b911558g · Cited by 35
Campbell, R. M., Cartwright, C. H., Chen, W., Chen, Y., Duzic, E., Fu, J., Loveland, M., Manning, R., McKibben, B. P., Pleiman, C. M., et al. (1999) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(99)00398-4 · Cited by 33
Self-citation[25] Fluorescence assays to study structure, dynamics, and function of RNA and RNA-ligand complexes
Walter, N. G., & Burke, J. M. (2000) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/s0076-6879(00)17027-2 · Cited by 33
A Flexible Data Analysis Tool for Chemical Genetic Screens
Kelley, B. P., Lunn, M. R., Root, D. E., Flaherty, S. P., Martino, A. M., & Stockwell, B. R. (2004) · Chemistry & Biology · doi:10.1016/j.chembiol.2004.08.026 · Cited by 32
Dunn, D. A., Orlowski, M., McCoy, P. M., Gastgeb, F., Appell, K., Ozgur, L., Webb, M. L., & Burbaum, J. J. (2000) · SLAS DISCOVERY · doi:10.1177/108705710000500310 · Cited by 32
Target-based drug discovery for the development of novel antiinfectives
Selzer, P. M., Brutsche, S., Wiesner, P., Schmid, P., & Müllner, H. (2000) · International Journal of Medical Microbiology · doi:10.1016/s1438-4221(00)80090-9 · Cited by 30
Automated affinity selection for rapid discovery of peptide binders
Zhang, G., Li, C., Quartararo, A. J., Loas, A., & Pentelute, B. L. (2021) · Chemical Science · doi:10.1039/d1sc02587b · Cited by 30
Villeneuve, L. (1999) · Biotechnology and Applied Biochemistry · doi:10.1111/j.1470-8744.1999.tb01153.x · Cited by 29
Tugendreich, S., Perkins, E. L., Couto, J., Barthmaier, P., Sun, D., Tang, S., Tulac, S., Nguyen, A., Yeh, E., Mays, A., et al. (2001) · Genome Research · doi:10.1101/gr.191601 · Cited by 29
“There has been widespread recognition that cell-based assays designed in model organisms such as the yeast Saccharomyces cerevisiae provide greater ease of genetic manipulation and can be screened rapidly at a low cost (Kirsch 1993; Silverman et al. 1998; Munder and Hinnen 1999).”
BackgroundYang, X., Wang, Y., Zhang, X., Chang, R., & Li, X. (2011) · Journal of Separation Science · doi:10.1002/jssc.201100366 · Cited by 28
Web resources for drug toxicity
Wolfgang, G. H. I., & Johnson, D. E. (2002) · Toxicology · doi:10.1016/s0300-483x(02)00022-7 · Cited by 28
Determining the optimal size of small molecule mixtures for high throughput NMR screening
Mercier, K., & Powers, R. (2005) · Journal of Biomolecular NMR · doi:10.1007/s10858-005-0948-4 · Cited by 28
“…of thousands to millions of compounds, which have evolved from decades worth of synthetic efforts, from acquisition or more recently from combinatorial chemistry approaches (Armstrong, 1999; Gonzalez and Negulescu, 1998; Oldenburg, 1998; Fernandes, 1998; Kenny et al., 1998; Silverman et al., 1998).”
BackgroundComparative virtual screening and novelty detection for NMDA-GlycineB antagonists
Krueger, B., Weil, T., & Schneider, G. (2009) · Journal of Computer-Aided Molecular Design · doi:10.1007/s10822-009-9304-1 · Cited by 27
“Due to the fact that HTS is a cost-intensive process [ 23 ] and hit rates of unfocused screening libraries are usually low [24], the concept of focused library design has received much interest [25‐27]: Screening candidates are pre-selected, e.g.”
BackgroundFrom genetics and genomics to drug discovery: yeast rises to the challenge
Mélèse, T., & Hieter, P. (2002) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(02)02097-7 · Cited by 27
Zhao, X., Nan, Y., Xiao, C., Zheng, J., Zheng, X., Wei, Y., & Zhang, Y. (2010) · Journal of Chromatography B · doi:10.1016/j.jchromb.2010.05.040 · Cited by 26
In Vivo Functional Assay of a Recombinant Aquaporin inPichia pastoris
Daniels, M., Wood, M. R., & Yeager, M. J. (2006) · Applied and Environmental Microbiology · doi:10.1128/aem.72.2.1507-1514.2006 · Cited by 26
“Our cell-based light absorbance test of aquaporin activity is more biologically relevant than a solution-based in vitro assay because the activity of a lead compound to its target is measured in vivo (51).”
BackgroundKhedkar, N. R., Sindkhedkar, M. D., & Joseph, A. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.108197 · Cited by 27
Interference by Naturally Occurring Fatty Acids in a Noncellular Enzyme-Based Aromatase Bioassay
Balunas, M. J., Su, B., Landini, S., Brueggemeier, R. W., & Kinghorn, A. D. (2006) · Journal of Natural Products · doi:10.1021/np050513p · Cited by 24
Applications of NMR to structure-based drug design in structural genomics
Powers, R. (2002) · Journal of Structural and Functional Genomics · doi:10.1023/a:1020445506369 · Cited by 24
Cell-Based Screening and Validation of Human Novel Genes Associated with Cell Viability
Wang, L., Gao, X., Gao, P., Deng, W., Yu, P., Ma, J., Guo, J., Wang, X., Cheng, H., Zhang, C., et al. (2006) · SLAS DISCOVERY · doi:10.1177/1087057106286654 · Cited by 24
Miniaturizing screening: how low can we go today?
Bossé, R., Illy, C., Elands, J., & Chelsky, D. (2000) · Drug Discovery Today · doi:10.1016/s1359-6446(00)01497-5 · Cited by 24
Kariv, I., Fereshteh, M., & Oldenburg, K. R. (2001) · SLAS DISCOVERY · doi:10.1177/108705710100600205 · Cited by 24
Modern methods of drug discovery: An introduction
Giersiefen, H., Hilgenfeld, R., & Hillisch, A. (2003) · Birkhäuser Basel eBooks · doi:10.1007/978-3-0348-7997-2_1 · Cited by 23
“Assays for HTS can be grouped into two categories: so-called solution-based biochemical assays and cell based assays [43, 44 ].”
MethodStructure Activity Relationship by NMR and by Computer: A Comparative Study
Sirockin, F., Sich, C., Improta, S., Schaefer, M., Saudek, V., Froloff, N., Karplus, M., & Dejaegere, A. P. (2002) · Journal of the American Chemical Society · doi:10.1021/ja0265658 · Cited by 24
Friedmann, Y., Shriki, A., Bennett, E. R., Golos, S., Diskin, R., Marbach, I., Bengal, E., & Engelberg, D. (2006) · Molecular Pharmacology · doi:10.1124/mol.106.022962 · Cited by 22
“The potential use of engineered yeast systems in screening for “hit compounds” for drug development has been proposed continuously in the last 20 years (Kirsch, 1993; Broach and Thorner, 1996; Pausch, 1997; Silverman et al., 1998; Munder and Hinnen, 1999; Young et al., 2004).”
BackgroundInfluentialEnomoto, K., Aono, Y., Mitsugi, T., Takahashi, K., Suzuki, R., Préaudat, M., Mathis, G., Kominami, G., & Takemoto, H. (2000) · SLAS DISCOVERY · doi:10.1177/108705710000500409 · Cited by 20
Turek-Etienne, T. C., Kober, T. P., Stafford, J. M., & Bryant, R. W. (2003) · Assay and Drug Development Technologies · doi:10.1089/154065803322302808 · Cited by 20
Ma, X., Wang, X., Gao, X., Wang, L., Yang, L., Gao, P., Deng, W., Yu, P., Ma, J., Guo, J., et al. (2007) · Life Sciences · doi:10.1016/j.lfs.2007.08.006 · Cited by 19
“Cell-based assays using reporter genes and fluorescence stains have proven effective for HTS, and have advantages such as high sensitivity, shorter assay duration, simple automation and fewer false positives from nonspecific interactions (Silverman et al., 1998; Dhundale and Goddard, 1996; Suto and Ignar, 1997; Entzer…”
Synthesis of cyclic sulfamoyl carbamates and ureas via ring-closing metathesis
Dougherty, J. M., Jiménez, M. D. S., & Hanson, P. R. (2005) · Tetrahedron · doi:10.1016/j.tet.2005.03.140 · Cited by 19
The STINT‐NMR Method for Studying In‐cell Protein‐Protein Interactions
Burz, D. S., & Shekhtman, A. G. (2010) · Current Protocols in Protein Science · doi:10.1002/0471140864.ps1711s61 · Cited by 18
Bian, Y., Huang, X., & Ren, J. (2016) · Analytical Methods · doi:10.1039/c5ay02844b · Cited by 17
High-throughput fluorescence polarization method for identifying ligands of LOX-11
Zhang, T., Huang, Z., Dai, Y., Chen, X., Zhu, P., & Du, G. (2006) · Acta Pharmacologica Sinica · doi:10.1111/j.1745-7254.2006.00281.x · Cited by 17
Green Fluorescent Protein Mutant as Label in Homogeneous Assays for Biomolecules
Deo, S. K., & Daunert, S. (2001) · Analytical Biochemistry · doi:10.1006/abio.2000.4909 · Cited by 17
Graf, S., Madigou, T., Li, R., Chesné, C., Stemmer, A., & Knapp, H. (2011) · JALA Journal of the Association for Laboratory Automation · doi:10.1016/j.jala.2011.03.006 · Cited by 16
“The current methods used for either transporting the substances through the cell membrane or inserting DNA, siRNA, mAbs, and other substances into living cells fall naturally into three categories: (1) chemical techniques that rely on carrier molecules; (2) viral vectors used by biologists to deliver genetic material…”
BackgroundMethodSasuga, S., Abe, R., Nikaido, O., Kiyosaki, S., Sekiguchi, H., Ikai, A., & Osada, T. (2012) · BioMed Research International · doi:10.1155/2012/804793 · Cited by 16
“Most yeast systems for the studying of GPCR signaling use reporter constructs to provide readouts for transcription from signal-dependent promoters and are used for clinical and pharmaceutical studies, for example, a drug screening, due to similarities between the yeast mating response pathway and human GPCR signal tr…”
BackgroundNonpeptide Ligands for Peptidergic G Protein-Coupled Receptors
Geary, T. G. (2010) · Advances in experimental medicine and biology · doi:10.1007/978-1-4419-6902-6_2 · Cited by 13
Mathematical Foundations and Biomechanics of the Digestive System
Miftahof, R. N., & Nam, H. G. (2010) · Cambridge University Press eBooks · doi:10.1017/cbo9780511711961 · Cited by 13
Han, H.-K., Sadagopan, N., Reichard, G. A., Yapa, U., Zhu, T., Hubbel, A., Johnson, K., & Brodfuehrer, J. (2006) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20642 · Cited by 13
Xi, Z., Khare, S., Cheung, A., Huang, B., Pan, T., Zhang, W., Ibrahim, F., Jin, C., & Gabos, S. (2014) · Computational Biology and Chemistry · doi:10.1016/j.compbiolchem.2013.12.004 · Cited by 12
Yang, Z., Fang, Z. D., He, W., Wang, Z., Gan, H., Tian, Q., & Guo, K. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.02.063 · Cited by 12
Basic Considerations in Designing High-Throughput Screening Assays
Bronson, D. D., Hentz, N. G., Janzen, W. P., Lister, M. D., Menke, K. C., Wegrzyn, J., & Sittampalam, G. S. (2001) · Drugs and the pharmaceutical sciences · doi:10.1201/9780203908570.ch2 · Cited by 12
Design and Implementation of High Throughput Screening Assays for Drug Discoveries
Bokhari, F. F., & Albukhari, A. (2021) · IntechOpen eBooks · doi:10.5772/intechopen.98733 · Cited by 11
Molecular Epidemiology of Human Cancer: Biomarkers of Genotoxic Exposure and Susceptibility
Grant, S. G. (2001) · Journal of Environmental Pathology Toxicology and Oncology · doi:10.1615/jenvironpatholtoxicoloncol.v20.i4.10 · Cited by 10
High‐Throughput Screening for Lead Discovery
Houston, J. G., & Banks, M. N. (2003) · Burger's Medicinal Chemistry and Drug Discovery · doi:10.1002/0471266949.bmc020 · Cited by 10
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