The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.
High-Throughput Screening in Drug Metabolism and Pharmacokinetic Support of Drug Discovery
Abstract
The application of rapid methods currently used for screening discovery drug candidates for metabolism and pharmacokinetic characteristics is discussed. General considerations are given for screening in this context, including the criteria for good screens, the use of counterscreens, the proper sequencing of screens, ambiguity in the interpretation of results, strategies for false positives and negatives, and the special difficulties encountered in drug metabolism and pharmacokinetic screening. Detailed descriptions of the present status of screening are provided for absorption potential, blood-brain barrier penetration, inhibition and induction of cytochrome P450, pharmacokinetics, biotransformation, and computer modeling. Although none of the systems currently employed for drug metabolism and pharmacokinetic screening can be considered truly high-throughput, several of them are rapid enough to be a practical part of the screening paradigm for modern, fast-moving discovery programs.
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Cites
Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00129-0 · Cited by 18,139
Kansy, M., Senner, F., & Gubernator, K. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm970530e · Cited by 1,304
Can We Learn To Distinguish between “Drug-like” and “Nondrug-like” Molecules?
Ajay, Walters, W. P., & Murcko, M. A. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm970666c · Cited by 484
A Scoring Scheme for Discriminating between Drugs and Nondrugs
Sadowski, J., & Kubinyi, H. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm9706776 · Cited by 392
Technological advances in high-throughput screening
Fernandes, P. B. (1998) · Current Opinion in Chemical Biology · doi:10.1016/s1367-5931(98)80089-6 · Cited by 170
New assay technologies for high-throughput screening
Silverman, L., Campbell, R., & Broach, J. R. (1998) · Current Opinion in Chemical Biology · doi:10.1016/s1367-5931(98)80015-x · Cited by 151
Lavé, T., Dupin, S., Schmitt, C., Valles, B., Ubeaud, G., Chou, R. C., Jaeck, D., & Coassolo, P. (1997) · Pharmaceutical Research · doi:10.1023/a:1012036324237 · Cited by 106
Cited by
Impact of Drug Transporter Studies on Drug Discovery and Development
Mizuno, N., Niwa, T., Yotsumoto, Y., & Sugiyama, Y. (2003) · Pharmacological Reviews · doi:10.1124/pr.55.3.1 · Cited by 490
SuFEx Click Chemistry Enabled Late-Stage Drug Functionalization
Liu, Z., Li, J., Li, S., Li, G., Sharpless, K. B., & Wu, P. (2018) · Journal of the American Chemical Society · doi:10.1021/jacs.7b12788 · Cited by 319
In vitro Tests for Predicting Drug‐Drug Interactions: The Need for Validated Procedures
Kremers, P. (2002) · Pharmacology & Toxicology · doi:10.1034/j.1600-0773.2002.910501.x · Cited by 41
Metadata
- Authors
- White, R. E.
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 2000-04
- Volume
- 40
- Issue
- 1
- Pages
- 133-157
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2116855266
- Cited by
- 304
- References
- 7
- FWCI
- 2.57
- Type
- journal article
- Language
- en
- Open access
- closed
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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