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Compound class: Natural product or derivative
Comment: Balanol is a fungal metabolite which acts as a non-selective ATP-competitive inhibitor of protein kinases A, G and C (AGC family kinases) [1-3]. Balanol is also reported to inhibit G protein-coupled receptor kinases (GRKs), with modest selectivity for the GRK2 family members, GRK2 and GRK3 .
Ligand Activity Visualisation Charts
These 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.✖
1. Defauw JM, Murphy MM, Jagdmann Jr GE, Hu H, Lampe JW, Hollinshead SP, Mitchell TJ, Crane HM, Heerding JM, Mendoza JS et al.. (1996)
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
J Med Chem, 39 (26): 5215-27. [PMID:8978850]
2. Koide K, Bunnage ME, Gomez Paloma L, Kanter JR, Taylor SS, Brunton LL, Nicolaou KC. (1995)
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.
Chem Biol, 2 (9): 601-8. [PMID:9383464]
3. Ohshima S, Yanagisawa M, Katoh A, Fujii T, Sano T, Matsukuma S, Furumai T, Fujiu M, Watanabe K, Yokose K et al.. (1994)
Fusarium merismoides Corda NR 6356, the source of the protein kinase C inhibitor, azepinostatin. Taxonomy, yield improvement, fermentation and biological activity.
J Antibiot, 47 (6): 639-47. [PMID:8040068]
4. Tesmer JJ, Tesmer VM, Lodowski DT, Steinhagen H, Huber J. (2010)
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J Med Chem, 53 (4): 1867-70. [PMID:20128603]