Synonyms: compound 11 [PMID: 24354345] | DNL-201 | DNL201 [2] | GNE0877
Compound class:
Synthetic organic
Comment: GNE-0877 (renamed DNL201; Denali Therapeutics) is a potent and selective, brain penetrant small molecule inhibitor of LRRK2 (leucine-rich repeat kinase 2) [1-2], a kinase whose aberrant activation is identified in a subset of patients with Parkinson's disease. LRRK2 ihnibitors are being developed as potential disease-modifying agents as therapeutics for Parkinson's disease. This mechanism is predicted to correct lysosomal dysfunction and neurodegenerative sequelae.
![]() 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. Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J et al.. (2014)
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem, 57 (3): 921-36. [PMID:24354345] |
2. Jennings D, Huntwork-Rodriguez S, Henry AG, Sasaki JC, Meisner R, Diaz D, Solanoy H, Wang X, Negrou E, Bondar VV et al.. (2022)
Preclinical and clinical evaluation of the LRRK2 inhibitor DNL201 for Parkinson's disease. Sci Transl Med, 14 (648): eabj2658. DOI: 10.1126/scitranslmed.abj2658 [PMID:35675433] |