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Compound class: Synthetic organic
Comment: The DDR1 and DDR2 receptor tyrosine kinases are new potential targets for anti-inflammatory drug discovery, as they are critical mediators of inflammatory cytokine secretion whose dysregulation is implicated in the progression of various human inflammatory diseases, including fibrosis, arthritis, atherosclerosis and cancer [1-2]. The dual inhibitor compound 5n was designed to investigate the anti-inflammatory potential of coinhibiting these enzymes, and provides a lead scaffold for further optimisation .
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. Borza CM, Pozzi A. (2014)
Discoidin domain receptors in disease.
Matrix Biol, 34: 185-92. [PMID:24361528]
2. Leitinger B. (2014)
Discoidin domain receptor functions in physiological and pathological conditions.
Int Rev Cell Mol Biol, 310: 39-87. [PMID:24725424]
3. Wang Z, Zhang Y, Pinkas DM, Fox AE, Luo J, Huang H, Cui S, Xiang Q, Xu T, Xun Q et al.. (2018)
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
J Med Chem, 61 (17): 7977-7990. [PMID:30075624]