Synonyms: AG-F-89549 | EVP4593
Compound class:
Synthetic organic
Comment: This compound potently inhibits nuclear factor-κB (NFκB) activation and LPS-induced TNFα production [7]. Its discovery is reported in [7] where it is compound 11q.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011)
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377] |
2. Baeuerle PA, Baltimore D. (1996)
NF-kappa B: ten years after. Cell, 87 (1): 13-20. [PMID:8858144] |
3. Baeuerle PA, Henkel T. (1994)
Function and activation of NF-kappa B in the immune system. Annu Rev Immunol, 12: 141-79. [PMID:8011280] |
4. Blackwell TS, Christman JW. (1997)
The role of nuclear factor-kappa B in cytokine gene regulation. Am J Respir Cell Mol Biol, 17 (1): 3-9. [PMID:9224203] |
5. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013)
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362] |
6. May MJ, Ghosh S. (1998)
Signal transduction through NF-kappa B. Immunol Today, 19 (2): 80-8. [PMID:9509763] |
7. Tobe M, Isobe Y, Tomizawa H, Nagasaki T, Takahashi H, Fukazawa T, Hayashi H. (2003)
Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation. Bioorg Med Chem, 11 (3): 383-91. [PMID:12517433] |
8. Vossen AC, Savelkoul HF. (1994)
Cytokines in clinical and experimental transplantation. Mediators Inflamm, 3 (6): 403-10. [PMID:18475587] |
9. Wu J, Shih HP, Vigont V, Hrdlicka L, Diggins L, Singh C, Mahoney M, Chesworth R, Shapiro G, Zimina O et al.. (2011)
Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment. Chem Biol, 18 (6): 777-93. [PMID:21700213] |