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Compound class: Peptide or derivative
Comment: DX600 is a peptide inhibitor of angiotensin-converting enzyme 2 (ACE2) . It blocks the cardioprotective effect of ACE2, but does not inhibit ACE activity [1-2].
A gallium-68 labeled cyclic DX600 derivative can be used as an ACE2 radiotracer 
SARS-CoV-2 and COVID-19: Experiments using lab-grown, human embryonic stem cell-derived beating cardiomyocytes have demonstrated that DX600 can prevent pseudotyped SARS-CoV-2 from entering the heart cells . This research indicates that agents that physically block spike-ACE2 binding could be leveraged as novel infection preventatives, that also offer the potential to reduce SARS-CoV-2-mediated damage to heart tissue.
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. Huang L, Sexton DJ, Skogerson K, Devlin M, Smith R, Sanyal I, Parry T, Kent R, Enright J, Wu QL et al.. (2003)
Novel peptide inhibitors of angiotensin-converting enzyme 2.
J Biol Chem, 278 (18): 15532-40. [PMID:12606557]
2. Joshi S, Balasubramanian N, Vasam G, Jarajapu YP. (2016)
Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells.
Eur J Pharmacol, 774: 25-33. [PMID:26851370]
3. Parker M, Blecha J, Rosenberg O, Ohliger M, Flavell RR, Wilson DM. (2021)
Cyclic gallium-68 labeled peptides for specific detection of human angiotensin-converting enzyme 2.
J Nucl Med, [Epub ahead of print]. DOI: 10.2967/jnumed.120.261768 [PMID:33637588]
4. Williams TL, Colzani MT, Macrae RGC, Robinson EL, Bloor S, Greenwood EJD, Zhan JR, Strachan G, Kuc RE, Nyimanu D et al.. (2021)
Human embryonic stem cell-derived cardiomyocyte platform screens inhibitors of SARS-CoV-2 infection.
Commun Biol, 4 (1): 926. [PMID:34326460]