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Synonyms: M6620 | VE 822 | VE-822 | VX-970 | VX970
Compound class: Synthetic organic
Comment: Berzosertib (VE-822) is a potent and selective inhibitor of the serine/threonine kinase ATR . The structure of VE-822 is claimed in patent US20130089626 . VE-822 is under investigated for its potential antineoplastic action .
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. Charrier JD, Durrant SJ, Golec JM, Kay DP, Knegtel RM, MacCormick S, Mortimore M, O'Donnell ME, Pinder JL, Reaper PM et al.. (2011)
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.
J. Med. Chem., 54 (7): 2320-30. [PMID:21413798]
2. Fokas E, Prevo R, Pollard JR, Reaper PM, Charlton PA, Cornelissen B, Vallis KA, Hammond EM, Olcina MM, Gillies McKenna W et al.. (2012)
Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation.
Cell Death Dis, 3: e441. [PMID:23222511]
3. Minchom A, Aversa C, Lopez J. (2018)
Dancing with the DNA damage response: next-generation anti-cancer therapeutic strategies.
Ther Adv Med Oncol, 10: 1758835918786658. [PMID:30023007]
4. Pollard JR, Reaper PM. (2013)
Treating Cancer with ATR Inhibitors.
Patent number: US20130089626. Assignee: Vertex Pharmaceuticals Incorporated. Priority date: 30/09/2011. Publication date: 11/04/2013.
5. Shi Q, Shen LY, Dong B, Fu H, Kang XZ, Yang YB, Dai L, Yan WP, Xiong HC, Liang Z et al.. (2018)
The identification of the ATR inhibitor VE-822 as a therapeutic strategy for enhancing cisplatin chemosensitivity in esophageal squamous cell carcinoma.
Cancer Lett., 432: 56-68. [PMID:29890208]