Synonyms: Daurismo® | PF 04449913 | PF-04449913
glasdegib is an approved drug (FDA (2018), EMA (2020))
Compound class:
Synthetic organic
Comment: Glasdegib is a potent and orally active inhibitor of the hedgehog signalling pathway, that acts as an antagonist of the class frizzled GPCR, smoothened (SMO) [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. Cortes JE, Douglas Smith B, Wang ES, Merchant A, Oehler VG, Arellano M, DeAngelo DJ, Pollyea DA, Sekeres MA, Robak T et al.. (2018)
Glasdegib in combination with cytarabine and daunorubicin in patients with AML or high-risk MDS: Phase 2 study results. Am J Hematol, 93 (11): 1301-1310. [PMID:30074259] |
2. Munchhof MJ, Li Q, Shavnya A, Borzillo GV, Boyden TL, Jones CS, LaGreca SD, Martinez-Alsina L, Patel N, Pelletier K et al.. (2012)
Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Med Chem Lett, 3 (2): 106-11. [PMID:24900436] |