Synonyms: GNF-PF-254
Compound class:
Synthetic organic
Comment: This is compound 5233705 in [4] (this is its ChemBridge reference). It was originally reported to be an AKT (protein kinase B) inhibitor [5]. However, the primary molecular target(s) of this compound have not been clearly identified, and its action may involve activation of the PDK1 kinase upstream of AKT, modulation of mTORC2 or targets outside of the PI3-kinase/AKT pathway [2].
PI3-kinase/AKT pathway inhibitors are under investigation as anticancer and antiviral agents. 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. Dunn EF, Fearns R, Connor JH. (2009)
Akt inhibitor Akt-IV blocks virus replication through an Akt-independent mechanism. J Virol, 83 (22): 11665-72. [PMID:19740993] |
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. Kau TR, Schroeder F, Ramaswamy S, Wojciechowski CL, Zhao JJ, Roberts TM, Clardy J, Sellers WR, Silver PA. (2003)
A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell, 4 (6): 463-76. [PMID:14706338] |
5. Sun Q, Wu R, Cai S, Lin Y, Sellers L, Sakamoto K, He B, Peterson BR. (2011)
Synthesis and biological evaluation of analogues of AKT (protein kinase B) inhibitor-IV. J Med Chem, 54 (5): 1126-39. [PMID:21319800] |