Compound class:
Synthetic organic
Comment: Compound 21 is a derivative synthesised and assessed in a medicinal chemistry study to identify potent small molecule inhibitors of receptor (TNFRSF)-interacting serine-threonine kinase 1 (RIPK1) [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. Galluzzi L, Kroemer G. (2011)
Necroptosis turns TNF lethal. Immunity, 35 (6): 849-51. [PMID:22195740] |
2. Harris PA, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Finger JN, Hoffman SJ, Kahler KM et al.. (2013)
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis. ACS Med Chem Lett, 4 (12): 1238-43. [PMID:24900635] |
3. Linkermann A, Bräsen JH, Himmerkus N, Liu S, Huber TB, Kunzendorf U, Krautwald S. (2012)
Rip1 (receptor-interacting protein kinase 1) mediates necroptosis and contributes to renal ischemia/reperfusion injury. Kidney Int, 81 (8): 751-61. [PMID:22237751] |
4. Pasparakis M, Vandenabeele P. (2015)
Necroptosis and its role in inflammation. Nature, 517 (7534): 311-20. [PMID:25592536] |
5. Rosenbaum DM, Degterev A, David J, Rosenbaum PS, Roth S, Grotta JC, Cuny GD, Yuan J, Savitz SI. (2010)
Necroptosis, a novel form of caspase-independent cell death, contributes to neuronal damage in a retinal ischemia-reperfusion injury model. J Neurosci Res, 88 (7): 1569-76. [PMID:20025059] |
6. Smith CC, Davidson SM, Lim SY, Simpkin JC, Hothersall JS, Yellon DM. (2007)
Necrostatin: a potentially novel cardioprotective agent?. Cardiovasc Drugs Ther, 21 (4): 227-33. [PMID:17665295] |
7. Trichonas G, Murakami Y, Thanos A, Morizane Y, Kayama M, Debouck CM, Hisatomi T, Miller JW, Vavvas DG. (2010)
Receptor interacting protein kinases mediate retinal detachment-induced photoreceptor necrosis and compensate for inhibition of apoptosis. Proc Natl Acad Sci USA, 107 (50): 21695-700. [PMID:21098270] |
8. Xu X, Chua KW, Chua CC, Liu CF, Hamdy RC, Chua BH. (2010)
Synergistic protective effects of humanin and necrostatin-1 on hypoxia and ischemia/reperfusion injury. Brain Res, 1355: 189-94. [PMID:20682300] |