Synonyms: M-4344 | M4344 | VX-803 | VX803
Compound class:
Synthetic organic
Comment: M4344 (VX-803) is a small molecule, ATP-competitive, selective and orally deliverable inhibitor of the DNA damage response pathway kinase, ataxia telangiectasia and rad3-related (ATR) [1]. The chemical structure of M4344 matches that for gartisertib, which was surfaced in WHO Proposed list 125 in July 2021.
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. ✖ |
|
References |
1. Jo U, Senatorov IS, Zimmermann A, Saha LK, Murai Y, Kim SH, Rajapakse VN, Elloumi F, Takahashi N, Schultz CW et al.. (2021)
Novel and Highly Potent ATR Inhibitor M4344 Kills Cancer Cells With Replication Stress, and Enhances the Chemotherapeutic Activity of Widely Used DNA Damaging Agents. Mol Cancer Ther, 20 (8): 1431-1441. [PMID:34045232] |
2. Zenke FT, Zimmermann A, Dahmen H, Elenbaas B, Pollard J, Reaper P, Bagrodia S, Spilker ME, Amendt C, Blaukat A.
Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Accessed on 28/07/2021. Modified on 28/07/2021. cancerres.aacrjournals.org, https://cancerres.aacrjournals.org/content/79/13_Supplement/369. DOI: 10.1158/1538-7445.AM2019-369 |