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Synonyms: AZ-1366 | compound 9 [PMID: 25815142]
Compound class: Synthetic organic
Comment: AZ1366 is an orally bioavailable inhibitor of the poly(ADP-ribose) polymerase (PARP) tankyrase enzymes TNKS and TNKS2 . It exhibits some activity against PARP1 and PARP2. Structurally it is a nicotinamide mimetic that occupies the nicotinamide binding site of the PARP catalytic domain.
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. Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL et al.. (2015)
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
ACS Med Chem Lett, 6 (3): 254-9. [PMID:25815142]
2. Quackenbush KS, Bagby S, Tai WM, Messersmith WA, Schreiber A, Greene J, Kim J, Wang G, Purkey A, Pitts TM et al.. (2016)
The novel tankyrase inhibitor (AZ1366) enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance.
Oncotarget, 7 (19): 28273-85. [PMID:27070088]
3. Scarborough HA, Helfrich BA, Casás-Selves M, Schuller AG, Grosskurth SE, Kim J, Tan AC, Chan DC, Zhang Z, Zaberezhnyy V et al.. (2017)
AZ1366: An Inhibitor of Tankyrase and the Canonical Wnt Pathway that Limits the Persistence of Non-Small Cell Lung Cancer Cells Following EGFR Inhibition.
Clin Cancer Res, 23 (6): 1531-1541. [PMID:27663586]