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Synonyms: LRRK2-IN1 | LRRK2IN1 
Compound class: Synthetic organic
Comment: LRRK2-IN-1 is a selective inhibitor of the Parkinson's associated kinase LRRK2 (leucine rich repeat kinase 2) . The compound has limited brain penetrance. LRRK2-IN-1 is used as a pharmacological tool to interrogate the function of LRRK2 in Parkinson's disease.
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.✖
|LRRK2-IN-1 inhibits activity of the LRRK2 G2019S activating mutation with an IC50 of 6nM . In patient derived lymphoblastoid cells and in mouse in vivo studies, treatment with LRRK2-IN-1 suppresses LRRK2 kinase activity resulting in dephosphorylation of Ser910 and Ser935 and loss of 14-3-3 binding with resultant re-distribution and accumulation of LRRK2 in aggregate fibrillar structures in the cytoplasm.
Kinase profile screening in biochemical assays identifies DCLK2, DCLK1 and MAPK7 as potential off-targets. LRRK1 inhibition could not be evaluated under the same assay conditions as LRRK2 inhibition .
|Selectivity at enzymes|
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