Compound class:
Synthetic organic
Comment: This is compound 72, an invention covered by patent WO2013026806 [5]. Compound 72 is a highly potent dual DYRK1A/1B inhibitor (DYRK = dual-specificity tyrosine-regulated kinase).
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 |
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A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro. J Neurochem, 133 (3): 440-51. [PMID:25556849] |
2. Ferrer I, Barrachina M, Puig B, Martínez de Lagrán M, Martí E, Avila J, Dierssen M. (2005)
Constitutive Dyrk1A is abnormally expressed in Alzheimer disease, Down syndrome, Pick disease, and related transgenic models. Neurobiol Dis, 20 (2): 392-400. [PMID:16242644] |
3. Foucourt A, Hédou D, Dubouilh-Benard C, Girard A, Taverne T, Casagrande AS, Désiré L, Leblond B, Besson T. (2014)
Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules, 19 (10): 15411-39. [PMID:25264830] |
4. Kimura R, Kamino K, Yamamoto M, Nuripa A, Kida T, Kazui H, Hashimoto R, Tanaka T, Kudo T, Yamagata H et al.. (2007)
The DYRK1A gene, encoded in chromosome 21 Down syndrome critical region, bridges between beta-amyloid production and tau phosphorylation in Alzheimer disease. Hum Mol Genet, 16 (1): 15-23. [PMID:17135279] |
5. Leblond B, Casagrande A-S, Desire L, Foucourt A, Besson T. (2013)
Dyrk1 inhibitors and uses thereof. Patent number: WO2013026806. Assignee: Exonhit Sa. Priority date: 19/08/2011. Publication date: 28/02/2013. |
6. Park J, Song WJ, Chung KC. (2009)
Function and regulation of Dyrk1A: towards understanding Down syndrome. Cell Mol Life Sci, 66 (20): 3235-40. [PMID:19685005] |
7. Ryoo SR, Jeong HK, Radnaabazar C, Yoo JJ, Cho HJ, Lee HW, Kim IS, Cheon YH, Ahn YS, Chung SH et al.. (2007)
DYRK1A-mediated hyperphosphorylation of Tau. A functional link between Down syndrome and Alzheimer disease. J Biol Chem, 282 (48): 34850-7. [PMID:17906291] |