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Synonyms: R-115777 | R115777
Compound class: Synthetic organic
Comment: Tipifarnib is a non-peptidomimetic competitive farnesyltransferase inhibitor (FTI) .
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. Angibaud P, Bourdrez X, Devine A, End DW, Freyne E, Ligny Y, Muller P, Mannens G, Pilatte I, Poncelet V et al.. (2003)
5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.
Bioorg Med Chem Lett, 13 (9): 1543-7. [PMID:12699751]
2. Downward J. (2003)
Targeting RAS signalling pathways in cancer therapy.
Nat Rev Cancer, 3 (1): 11-22. [PMID:12509763]
3. End DW, Smets G, Todd AV, Applegate TL, Fuery CJ, Angibaud P, Venet M, Sanz G, Poignet H, Skrzat S et al.. (2001)
Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.
Cancer Res, 61 (1): 131-7. [PMID:11196150]
4. Venet M, End D, Angibaud P. (2003)
Farnesyl protein transferase inhibitor ZARNESTRA R115777 - history of a discovery.
Curr Top Med Chem, 3 (10): 1095-102. [PMID:12769710]