Synonyms: compound 6 [PMID: 37591317]
Compound class:
Synthetic organic
Comment: JH-XII-03-02 is a LRRK2 PROTAC degrader molecule [1]. It simultaneously inhibits LRRK2 kinase activity and disrupts LRRK2's scaffolding function. Reducing LRRK2 activity is being investigated for potential to treat Parkinson's disease that is caused by inherited LRRK2 mutations. JH-XII-03-02 promotes cereblon-mediated degradation of LRRK2.
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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Bioactivity Comments |
JH-XII-03-02 retains LRRK2 inhibition potency for wild type LRRK2 and LRRK2G2019S, and it is highly selective for LRRK2 in a KINOMEscan [1]. In a cell-based assay 1μM JH-XII-03-02 almost completely degrades LRRK2 protein after 48 hours incubation. |
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