Synonyms: ryuvidine
Compound class:
Synthetic organic
Comment: CDK4 inhibitor III (ryuvidine), as its name suggests was originally reported as a selective inhibitor of CDK4, albeit a weak inhibitor [6]. However, to date (October 2018) there is no published data showing cellular inhibition of CDK4 by this compound, but some evidence of action at another target(s) that regulates the S phase of the cell cycle has been reported [5]. This latter effect may be due to CDK4 inhibitor III-induced inhibition of the lysine methyltransferase SETD8 [2,4].
![]() 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. Blum G, Ibáñez G, Rao X, Shum D, Radu C, Djaballah H, Rice JC, Luo M. (2014)
Small-molecule inhibitors of SETD8 with cellular activity. ACS Chem Biol, 9 (11): 2471-8. [PMID:25137013] |
3. 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] |
4. Houston SI, McManus KJ, Adams MM, Sims JK, Carpenter PB, Hendzel MJ, Rice JC. (2008)
Catalytic function of the PR-Set7 histone H4 lysine 20 monomethyltransferase is essential for mitotic entry and genomic stability. J Biol Chem, 283 (28): 19478-88. [PMID:18480059] |
5. Jorda R, Hendrychová D, Voller J, Řezníčková E, Gucký T, Kryštof V. (2018)
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem, 61 (20): 9105-9120. [PMID:30234987] |
6. Ryu CK, Kang HY, Lee SK, Nam KA, Hong CY, Ko WG, Lee BH. (2000)
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg Med Chem Lett, 10 (5): 461-4. [PMID:10743948] |