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Compound class: Synthetic organic
Comment: J30-8 is a selective JNK3 (a.k.a. mitogen-activated protein kinase 10; MAPK10) inhibitor. It is the most potent inhibitor from a series of compounds reported by Dou et al. (2019) that were identified using structure-based virtual, similarity and SAR screening stages . JNK3 has been proposed as the primary kinase that is responsible for phosphorylating Aβ precursor protein (APP) at Thr668, which leads to accelerated Aβ formation and elevated plaque burden [1,3]. Pharmacological inhibition of JNK3 is therefore being explored as a novel modality for the treatment of Alzheimer's and other neurodegenerative diseases. J30-8 provides a suitable in vitro and in vivo tool to further study JNK3's role in these pathological conditions.
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. Colombo A, Bastone A, Ploia C, Sclip A, Salmona M, Forloni G, Borsello T. (2009)
JNK regulates APP cleavage and degradation in a model of Alzheimer's disease.
Neurobiol Dis, 33 (3): 518-25. [PMID:19166938]
2. Dou X, Huang H, Li Y, Jiang L, Wang Y, Jin H, Jiao N, Zhang L, Zhang L, Liu Z. (2019)
Multistage Screening Reveals 3-Substituted Indolin-2-one Derivatives as Novel and Isoform-Selective c-Jun N-terminal Kinase 3 (JNK3) Inhibitors: Implications to Drug Discovery for Potential Treatment of Neurodegenerative Diseases.
J Med Chem, 62 (14): 6645-6664. [PMID:31268308]
3. Triaca V, Sposato V, Bolasco G, Ciotti MT, Pelicci P, Bruni AC, Cupidi C, Maletta R, Feligioni M, Nisticò R et al.. (2016)
NGF controls APP cleavage by downregulating APP phosphorylation at Thr668: relevance for Alzheimer's disease.
Aging Cell, 15 (4): 661-72. [PMID:27076121]