Synonyms: BX 795 | BX795
Compound class:
Synthetic organic
Comment: BX-795 is a potent, ATP-competitive inhibitor of 3-phosphoinositide dependent protein kinase 1 (PDK1). The discovery of BX-795 is described in [3] and is claimed in patent WO2004048343 [1]. The PDK1/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumour angiogenesis and represents a promising target for oncology therapeutics. BX-795 has subsequently been discovered to inhibit other kinases, such as TANK-binding kinase 1 (TBK1) and IkappaB kinase epsilon (IKKε) [2].
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. Arnaiz D, Boemer U, Briem H, Bryant J, Buckman B, Eckle E, Esperling P, Feldman R, Huwe P, Khim S-K et al.. (2004)
Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents. Patent number: WO2004048343. Assignee: Schering Ag. Priority date: 28/11/2002. Publication date: 10/06/2004. |
2. Clark K, Plater L, Peggie M, Cohen P. (2009)
Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem, 284 (21): 14136-46. [PMID:19307177] |
3. Feldman RI, Wu JM, Polokoff MA, Kochanny MJ, Dinter H, Zhu D, Biroc SL, Alicke B, Bryant J, Yuan S et al.. (2005)
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem, 280 (20): 19867-74. [PMID:15772071] |
4. Hasan M, Yan N. (2016)
Therapeutic potential of targeting TBK1 in autoimmune diseases and interferonopathies. Pharmacol Res, 111: 336-42. [PMID:27353409] |