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Compound class: Synthetic organic
Comment: FRAX486 is a brain penetrant and orally bioavailable inhibitor of group 1 p21 protein (Cdc42/Rac)-activated kinases (PAK1, PAK2 and PAK3; PAKA subfamily) . Experimental evidence suggests inhibition of PAKs may offer neuroprotective [2-3] and anti-cancer potential.
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. Dittmar M, Lee JS, Whig K, Segrist E, Li M, Kamalia B, Castellana L, Ayyanathan K, Cardenas-Diaz FL, Morrisey EE et al.. (2021)
Drug repurposing screens reveal cell-type-specific entry pathways and FDA-approved drugs active against SARS-Cov-2.
Cell Rep,: 108959 [Epub ahead of print]. [PMID:33811811]
2. Dolan BM, Duron SG, Campbell DA, Vollrath B, Shankaranarayana Rao BS, Ko HY, Lin GG, Govindarajan A, Choi SY, Tonegawa S. (2013)
Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486.
Proc Natl Acad Sci USA, 110 (14): 5671-6. [PMID:23509247]
3. Hayashi-Takagi A, Araki Y, Nakamura M, Vollrath B, Duron SG, Yan Z, Kasai H, Huganir RL, Campbell DA, Sawa A. (2014)
PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence.
Proc Natl Acad Sci USA, 111 (17): 6461-6. [PMID:24706880]