The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery
Open accessAbstract
More than 500 compounds chosen to represent kinase inhibitor space have been screened against a panel of over 200 protein kinases. Significant results include the identification of hits against new kinases including PIM1 and MPSK1, and the expansion of the inhibition profiles of several literature compounds. A detailed analysis of the data through the use of affinity fingerprints has produced findings with implications for biological target selection, the choice of tool compounds for target validation, and lead discovery and optimization. In a detailed examination of the tyrosine kinases, interesting relationships have been found between targets and compounds. Taken together, these results show how broad cross-profiling can provide important insights to assist kinase drug discovery.
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Cites
A quantitative analysis of kinase inhibitor selectivity
Karaman, M. W., Herrgard, S., Treiber, D. K., Gallant, P., Atteridge, C. E., Campbell, B. T., Chan, K. W., Ciceri, P., Davis, M. I., Edeen, P. T., et al. (2008) · Nature Biotechnology · doi:10.1038/nbt1358 · Cited by 2,466
The specificities of protein kinase inhibitors: an update
BAIN, J., McLAUCHLAN, H., ELLIOTT, M., & COHEN, P. (2003) · Biochemical Journal · doi:10.1042/bj20021535 · Cited by 1,369
Cited by
Comprehensive analysis of kinase inhibitor selectivity
Davis, M. I., Hunt, J. P., Herrgard, S., Ciceri, P., Wodicka, L. M., Pallares, G., Hocker, M., Treiber, D. K., & Zarrinkar, P. P. (2011) · Nature Biotechnology · doi:10.1038/nbt.1990 · Cited by 2,409
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
Anastassiadis, T., Deacon, S. W., Devarajan, K., Ma, H., & Peterson, J. R. (2011) · Nature Biotechnology · doi:10.1038/nbt.2017 · Cited by 919
Targeting the cancer kinome through polypharmacology
Knight, Z. A., Lin, H., & Shokat, K. M. (2010) · Nature reviews. Cancer · doi:10.1038/nrc2787 · Cited by 674
Multiplexed mass cytometry profiling of cellular states perturbed by small-molecule regulators
Bodenmiller, B., Zunder, E. R., Finck, R., Chen, T. J., Savig, E. S., Bruggner, R. V., Simonds, E. F., Bendall, S. C., Sachs, K., Krutzik, P. O., et al. (2012) · Nature Biotechnology · doi:10.1038/nbt.2317 · Cited by 546
Targeting Mitosis in Cancer: Emerging Strategies
Dominguez-Brauer, C., Thu, K. L., Mason, J. M., Blaser, H., Bray, M. R., & Mak, T. W. (2015) · Molecular Cell · doi:10.1016/j.molcel.2015.11.006 · Cited by 495
Metadata
- Authors
- Bamborough, P., Drewry, D., Harper, G., Smith, G. K., & Schneider, K.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-11-26
- Volume
- 51
- Issue
- 24
- Pages
- 7898-7914
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1989116199
- Cited by
- 158
- References
- 2
- FWCI
- 20.47
- Type
- journal article
- Language
- en
- Open access
- green
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- Bamborough, P., Drewry, D., Harper, G., Smith, G. K., & Schneider, K. (2008). Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm8011036
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